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Sorafenib (BAY 43-9006) Raf/VEGFR inhibitor

Name: Sorafenib (BAY 43-9006)
Brand: Selleck Chemicals
SKU: S7397
Rating: 5 (580 reviews)

Cat.No.S7397

Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.

Chemical Structure

Molecular Weight: 464.82

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Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	ERK p38 MAPK JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Other Raf Inhibitors	LY3009120 Exarafenib (KIN-2787) GDC-0879 Avutometinib (Ro5126766, CH5126766) PLX-4720 AZ 628 SB590885 TAK-632 GW5074 RAF265 (CHIR-265)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	PMID
MV-4-11	Growth Inhibition Assay	IC50=0.00000303 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay	IC50=0.00418 μM	SANGER
ALL-PO	Growth Inhibition Assay	IC50=0.03184 μM	SANGER
NKM-1	Growth Inhibition Assay	IC50=0.07416 μM	SANGER
CGTH-W-1	Growth Inhibition Assay	IC50=0.25022 μM	SANGER
BB65-RCC	Growth Inhibition Assay	IC50=0.47073 μM	SANGER
NOS-1	Growth Inhibition Assay	IC50=0.5636 μM	SANGER
SH-4	Growth Inhibition Assay	IC50=0.65613 μM	SANGER
HOP-62	Growth Inhibition Assay	IC50=0.85088 μM	SANGER
HCC2998	Growth Inhibition Assay	IC50=0.88818 μM	SANGER
GDM-1	Growth Inhibition Assay	IC50=0.90698 μM	SANGER
KM12	Growth Inhibition Assay	IC50=1.02098 μM	SANGER
LB2518-MEL	Growth Inhibition Assay	IC50=1.20809 μM	SANGER
NCI-H1436	Growth Inhibition Assay	IC50=1.21678 μM	SANGER
EM-2	Growth Inhibition Assay	IC50=1.35578 μM	SANGER
LAMA-84	Growth Inhibition Assay	IC50=1.37648 μM	SANGER
KG-1	Growth Inhibition Assay	IC50=1.47935 μM	SANGER
A388	Growth Inhibition Assay	IC50=1.59165 μM	SANGER
no-10	Growth Inhibition Assay	IC50=1.61726 μM	SANGER
SF126	Growth Inhibition Assay	IC50=1.63812 μM	SANGER
MEG-01	Growth Inhibition Assay	IC50=1.8098 μM	SANGER
A3-KAW	Growth Inhibition Assay	IC50=1.8842 μM	SANGER
D-247MG	Growth Inhibition Assay	IC50=2.1448 μM	SANGER
OVCAR-4	Growth Inhibition Assay	IC50=2.21393 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay	IC50=2.3162 μM	SANGER
NCI-H2171	Growth Inhibition Assay	IC50=2.39764 μM	SANGER
SIG-M5	Growth Inhibition Assay	IC50=2.42242 μM	SANGER
BE-13	Growth Inhibition Assay	IC50=2.69609 μM	SANGER
K052	Growth Inhibition Assay	IC50=2.74616 μM	SANGER
L-540	Growth Inhibition Assay	IC50=2.75789 μM	SANGER
KMOE-2	Growth Inhibition Assay	IC50=2.8135 μM	SANGER
MFH-ino	Growth Inhibition Assay	IC50=2.92185 μM	SANGER
HL-60	Growth Inhibition Assay	IC50=3.06299 μM	SANGER
HCC2218	Growth Inhibition Assay	IC50=3.12003 μM	SANGER
TE-5	Growth Inhibition Assay	IC50=3.13162 μM	SANGER
MZ1-PC	Growth Inhibition Assay	IC50=3.47509 μM	SANGER
MRK-nu-1	Growth Inhibition Assay	IC50=3.61468 μM	SANGER
MZ7-mel	Growth Inhibition Assay	IC50=3.66099 μM	SANGER
BC-1	Growth Inhibition Assay	IC50=3.7402 μM	SANGER
ST486	Growth Inhibition Assay	IC50=3.83673 μM	SANGER
KS-1	Growth Inhibition Assay	IC50=3.88198 μM	SANGER
SK-NEP-1	Growth Inhibition Assay	IC50=4.16815 μM	SANGER
BC-3	Growth Inhibition Assay	IC50=4.23391 μM	SANGER
NCI-H1581	Growth Inhibition Assay	IC50=4.28798 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay	IC50=4.40484 μM	SANGER
NOMO-1	Growth Inhibition Assay	IC50=4.48905 μM	SANGER
QIMR-WIL	Growth Inhibition Assay	IC50=5.07294 μM	SANGER
SF539	Growth Inhibition Assay	IC50=5.13227 μM	SANGER
TE-12	Growth Inhibition Assay	IC50=5.24929 μM	SANGER
NCI-H510A	Growth Inhibition Assay	IC50=5.41685 μM	SANGER
JAR	Growth Inhibition Assay	IC50=5.50824 μM	SANGER
no-11	Growth Inhibition Assay	IC50=5.73568 μM	SANGER
BV-173	Growth Inhibition Assay	IC50=5.95682 μM	SANGER
SR	Growth Inhibition Assay	IC50=6.00678 μM	SANGER
MOLT-16	Growth Inhibition Assay	IC50=6.25266 μM	SANGER
MZ2-MEL	Growth Inhibition Assay	IC50=6.31839 μM	SANGER
SW954	Growth Inhibition Assay	IC50=6.45866 μM	SANGER
ML-2	Growth Inhibition Assay	IC50=6.52849 μM	SANGER
OCI-AML2	Growth Inhibition Assay	IC50=6.61062 μM	SANGER
SIMA	Growth Inhibition Assay	IC50=7.00101 μM	SANGER
DOHH-2	Growth Inhibition Assay	IC50=7.05676 μM	SANGER
697	Growth Inhibition Assay	IC50=7.05989 μM	SANGER
NB1	Growth Inhibition Assay	IC50=7.40407 μM	SANGER
D-392MG	Growth Inhibition Assay	IC50=7.62663 μM	SANGER
ES8	Growth Inhibition Assay	IC50=7.76503 μM	SANGER
RPMI-8226	Growth Inhibition Assay	IC50=7.84511 μM	SANGER
IST-MEL1	Growth Inhibition Assay	IC50=8.40002 μM	SANGER
NB14	Growth Inhibition Assay	IC50=8.63133 μM	SANGER
HD-MY-Z	Growth Inhibition Assay	IC50=8.63746 μM	SANGER
TE-10	Growth Inhibition Assay	IC50=8.76353 μM	SANGER
LC-1F	Growth Inhibition Assay	IC50=9.10834 μM	SANGER
OS-RC-2	Growth Inhibition Assay	IC50=9.11243 μM	SANGER
NCI-SNU-16	Growth Inhibition Assay	IC50=9.21026 μM	SANGER
SHP-77	Growth Inhibition Assay	IC50=9.71662 μM	SANGER
A4-Fuk	Growth Inhibition Assay	IC50=9.7561 μM	SANGER
NB6	Growth Inhibition Assay	IC50=9.76029 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay	IC50=10.4745 μM	SANGER
DMS-114	Growth Inhibition Assay	IC50=10.5441 μM	SANGER
NB7	Growth Inhibition Assay	IC50=10.7526 μM	SANGER
NCI-H747	Growth Inhibition Assay	IC50=11.1216 μM	SANGER
HH	Growth Inhibition Assay	IC50=11.3876 μM	SANGER
EW-18	Growth Inhibition Assay	IC50=11.9044 μM	SANGER
CHP-126	Growth Inhibition Assay	IC50=11.9738 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay	IC50=12.0278 μM	SANGER
DEL	Growth Inhibition Assay	IC50=12.0985 μM	SANGER
LU-139	Growth Inhibition Assay	IC50=12.5413 μM	SANGER
P30-OHK	Growth Inhibition Assay	IC50=12.5479 μM	SANGER
NCI-H1522	Growth Inhibition Assay	IC50=12.746 μM	SANGER
NCI-H1299	Growth Inhibition Assay	IC50=13.2911 μM	SANGER
UACC-257	Growth Inhibition Assay	IC50=13.5126 μM	SANGER
Calu-6	Growth Inhibition Assay	IC50=13.6046 μM	SANGER
NCI-H1882	Growth Inhibition Assay	IC50=13.8555 μM	SANGER
BB30-HNC	Growth Inhibition Assay	IC50=14.0609 μM	SANGER
ES1	Growth Inhibition Assay	IC50=14.1551 μM	SANGER
NCI-H1694	Growth Inhibition Assay	IC50=14.4811 μM	SANGER
IST-SL1	Growth Inhibition Assay	IC50=14.9616 μM	SANGER
ECC4	Growth Inhibition Assay	IC50=15.0558 μM	SANGER
MDA-MB-134-VI	Growth Inhibition Assay	IC50=15.4131 μM	SANGER
SCH	Growth Inhibition Assay	IC50=15.4728 μM	SANGER
SK-N-FI	Growth Inhibition Assay	IC50=15.6534 μM	SANGER
HDLM-2	Growth Inhibition Assay	IC50=16.0714 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay	IC50=16.1297 μM	SANGER
EW-24	Growth Inhibition Assay	IC50=16.1661 μM	SANGER
NCI-H2141	Growth Inhibition Assay	IC50=16.189 μM	SANGER
LC4-1	Growth Inhibition Assay	IC50=16.6119 μM	SANGER
HT-144	Growth Inhibition Assay	IC50=17.006 μM	SANGER
SK-MEL-1	Growth Inhibition Assay	IC50=17.0072 μM	SANGER
SCC-15	Growth Inhibition Assay	IC50=17.1638 μM	SANGER
C8166	Growth Inhibition Assay	IC50=17.6833 μM	SANGER
GOTO	Growth Inhibition Assay	IC50=17.8344 μM	SANGER
COR-L279	Growth Inhibition Assay	IC50=18.1362 μM	SANGER
K-562	Growth Inhibition Assay	IC50=18.7143 μM	SANGER
ES3	Growth Inhibition Assay	IC50=18.8041 μM	SANGER
LU-165	Growth Inhibition Assay	IC50=19.7008 μM	SANGER
KM-H2	Growth Inhibition Assay	IC50=20.3184 μM	SANGER
RL	Growth Inhibition Assay	IC50=20.9692 μM	SANGER
EW-3	Growth Inhibition Assay	IC50=21.1889 μM	SANGER
A101D	Growth Inhibition Assay	IC50=21.3752 μM	SANGER
HUTU-80	Growth Inhibition Assay	IC50=21.3946 μM	SANGER
NCI-H23	Growth Inhibition Assay	IC50=21.3992 μM	SANGER
PF-382	Growth Inhibition Assay	IC50=21.4403 μM	SANGER
LB373-MEL-D	Growth Inhibition Assay	IC50=21.5615 μM	SANGER
TE-8	Growth Inhibition Assay	IC50=21.6394 μM	SANGER
TE-9	Growth Inhibition Assay	IC50=21.8513 μM	SANGER
Daudi	Growth Inhibition Assay	IC50=21.9304 μM	SANGER
D-542MG	Growth Inhibition Assay	IC50=22.0256 μM	SANGER
U-698-M	Growth Inhibition Assay	IC50=22.4603 μM	SANGER
ES6	Growth Inhibition Assay	IC50=22.7366 μM	SANGER
DU-4475	Growth Inhibition Assay	IC50=23.8897 μM	SANGER
ECC12	Growth Inhibition Assay	IC50=24.2803 μM	SANGER
C2BBe1	Growth Inhibition Assay	IC50=24.3239 μM	SANGER
IST-SL2	Growth Inhibition Assay	IC50=24.4362 μM	SANGER
DJM-1	Growth Inhibition Assay	IC50=24.5221 μM	SANGER
DMS-153	Growth Inhibition Assay	IC50=24.8614 μM	SANGER
NB13	Growth Inhibition Assay	IC50=25.0265 μM	SANGER
SK-N-DZ	Growth Inhibition Assay	IC50=26.3414 μM	SANGER
COR-L88	Growth Inhibition Assay	IC50=26.5796 μM	SANGER
LU-65	Growth Inhibition Assay	IC50=26.8535 μM	SANGER
TGBC1TKB	Growth Inhibition Assay	IC50=26.9828 μM	SANGER
THP-1	Growth Inhibition Assay	IC50=27.2141 μM	SANGER
ONS-76	Growth Inhibition Assay	IC50=27.332 μM	SANGER
LC-2-ad	Growth Inhibition Assay	IC50=27.6231 μM	SANGER
EW-13	Growth Inhibition Assay	IC50=29.1746 μM	SANGER
MS-1	Growth Inhibition Assay	IC50=30.7278 μM	SANGER
NCI-H2227	Growth Inhibition Assay	IC50=30.9806 μM	SANGER
LXF-289	Growth Inhibition Assay	IC50=31.4492 μM	SANGER
MC116	Growth Inhibition Assay	IC50=32.0826 μM	SANGER
EVSA-T	Growth Inhibition Assay	IC50=32.2585 μM	SANGER
CTB-1	Growth Inhibition Assay	IC50=33.1101 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay	IC50=33.1603 μM	SANGER
NCI-H2196	Growth Inhibition Assay	IC50=33.2557 μM	SANGER
LB2241-RCC	Growth Inhibition Assay	IC50=33.3135 μM	SANGER
LS-513	Growth Inhibition Assay	IC50=33.8638 μM	SANGER
LP-1	Growth Inhibition Assay	IC50=33.9956 μM	SANGER
A253	Growth Inhibition Assay	IC50=34.2296 μM	SANGER
SK-MM-2	Growth Inhibition Assay	IC50=34.9451 μM	SANGER
NCI-H1963	Growth Inhibition Assay	IC50=35.3072 μM	SANGER
MMAC-SF	Growth Inhibition Assay	IC50=35.8785 μM	SANGER
LB831-BLC	Growth Inhibition Assay	IC50=36.0654 μM	SANGER
WSU-NHL	Growth Inhibition Assay	IC50=36.164 μM	SANGER
CESS	Growth Inhibition Assay	IC50=36.2848 μM	SANGER
NEC8	Growth Inhibition Assay	IC50=36.5835 μM	SANGER
KNS-42	Growth Inhibition Assay	IC50=37.1237 μM	SANGER
MHH-CALL-2	Growth Inhibition Assay	IC50=37.1821 μM	SANGER
K5	Growth Inhibition Assay	IC50=38.43 μM	SANGER
CP66-MEL	Growth Inhibition Assay	IC50=39.0733 μM	SANGER
OPM-2	Growth Inhibition Assay	IC50=39.8432 μM	SANGER
IST-MES1	Growth Inhibition Assay	IC50=40.3096 μM	SANGER
EC-GI-10	Growth Inhibition Assay	IC50=41.5805 μM	SANGER
CTV-1	Growth Inhibition Assay	IC50=42.8406 μM	SANGER
DG-75	Growth Inhibition Assay	IC50=43.7595 μM	SANGER
KNS-81-FD	Growth Inhibition Assay	IC50=45.4058 μM	SANGER
NCI-H82	Growth Inhibition Assay	IC50=45.5758 μM	SANGER
RPMI-8866	Growth Inhibition Assay	IC50=46.1873 μM	SANGER
ACN	Growth Inhibition Assay	IC50=46.434 μM	SANGER
NCI-H1395	Growth Inhibition Assay	IC50=46.4756 μM	SANGER
NCI-H209	Growth Inhibition Assay	IC50=47.1405 μM	SANGER
TGW	Growth Inhibition Assay	IC50=49.0791 μM	SANGER
NCI-H748	Growth Inhibition Assay	IC50=49.4753 μM	SANGER
EKVX	Growth Inhibition Assay	IC50=49.6628 μM	SANGER
MV4-11	Antiproliferative activity assay	IC50 = 0.00087 μM	19754199
MV4-11	Cytotoxicity assay	IC50 = 0.00087 μM	19654408
TT	Antiproliferative activity assay	IC50 = 0.0014 μM	18849971
RS4-11	Function assay	IC50 = 0.002 μM	19654408
MOLM13	Function assay	IC50 = 0.002 μM	24641103
Sf9	Function assay	IC50 = 0.003 μM	21708468
RS4-11	Function assay	IC50 = 0.0032 μM	19654408
MV4-11	Growth inhibition assay	IC50 = 0.004 μM	29357250
A375	Function assay	IC50 = 0.0044 μM	29461827
MOLM13	Antiproliferative activity assay	IC50 = 0.005 μM	24641103
MV4-11	Function assay	IC50 = 0.007 μM	23362959
MV4-11	Cytotoxicity assay	IC50 = 0.007 μM	26342867
HEK293	Function assay	Kd = 0.013 μM	19754199
Kasumi-1	Antiproliferative activity assay	IC50 = 0.015 μM	20570526
MV4-11	Antiproliferative activity assay	IC50 = 0.015 μM	20570526
sf9	Function assay	IC50 = 0.015 μM	29266937
sf9	Function assay	IC50 = 0.018 μM	21708468
sf9	Function assay	IC50 = 0.02 μM	23618709
MV4-11	Antiproliferative activity assay	GI50 = 0.03 μM	21708468
Sf9	Function assay	IC50 = 0.042 μM	26081023
SF9	Function assay	IC50 = 0.043 μM	18473434
MV4-11	Cytotoxicity assay	GI50 = 0.043 μM	23618709
MV4-11	Function assay	GI50 = 0.043 μM	26081023
SF9	Function assay	IC50 = 0.044 μM	26081023
SF9	Function assay	IC50 = 0.054 μM	21708468
SF9	Function assay	IC50 = 0.054 μM	23618709
MOLM13	Antiproliferative activity assay	GI50 = 0.056 μM	21708468
MOLM13	Antiproliferative activity assay	GI50 = 0.056 μM	22726931
MOLM13	Cytotoxicity assay	GI50 = 0.056 μM	23618709
MOLM-13	Function assay	GI50 = 0.056 μM	26081023
SF9	Function assay	IC50 = 0.058 μM	29266937
WM266.4	Antiproliferative activity assay	IC50 = 0.06 μM	25496804
MDA-MB-231	Function assay	IC50 = 0.063 μM	28431342
SF9	Function assay	IC50 = 0.09 μM	29266937
Spodoptera frugiperda	Function assay	IC50 = 0.09 μM	26922228
SF9	Function assay	IC50 = 0.09 μM	23562241
SF9	Function assay	IC50 = 0.1 μM	23442188
SF9	Function assay	IC50 = 0.1 μM	23442188
HEK293	Function assay	IC50 = 0.12 μM	26318998
MCF7	Antiproliferative activity assay	IC50 = 0.19 μM	25496804
MV4-11	Antiproliferative activity human	IC50 = 0.3 μM	28242553
HepG2	Antiproliferative activity assay	EC50 = 0.302 μM	27010810
THP1	Antiproliferative activity assay	IC50 = 0.31 μM	20570526
SMMC7721	Cytotoxicity assay	IC50 = 0.37 μM	25982075
HT-29	Antiproliferative activity assay	IC50 = 0.39 μM	25778995
sf9	Function assay	Kd = 0.6 μM	28109791
T47D	Antiproliferative activity assay	IC50 = 0.61 μM	25778995
A549	Cytotoxicity assay	IC50 = 0.63 μM	25982075
HeLa	Cytotoxicity assay	IC50 = 0.64 μM	30015070
WM3629	Antiproliferative activity assay	GI50 = 0.65 μM	20466542
SMMC7721	Antiproliferative activity assay	IC50 = 0.65 μM	26342134
WM3629	Growth inhibition assay	GI50 = 0.78 μM	20149658
WM3629	Antiproliferative activity assay	GI50 = 0.78 μM	26810260
MCF7	Antiproliferative activity assay	IC50 = 0.78 μM	25778995
K562	Antiproliferative activity assay	IC50 = 0.86 μM	24315192
COLO205	Antiproliferative activity assay	IC50 = 0.87 μM	25778995
T29	Cytotoxicity assay	IC50 = 0.9 μM	26318998
MDA-MB-231	Cytotoxicity assay	IC50 = 0.94 μM	25086238
MDA-MB-231	Cytotoxicity assay	IC50 = 0.94 μM	25440879
HepG2	Antiproliferative activity assay	IC50 = 1.06 μM	29628325
BL21(DE3)	Function assay	IC50 = 1.1 μM	19928858
K562	Antiproliferative activity assay	IC50 = 1.22 μM	25778995
MDA-MB-231	Growth inhibition assay	GI50 = 1.26 μM	28088086
MDA-MB-231	Cytotoxicity assay	GI50 = 1.26 μM	26590508
MDA-MB-231	Antiproliferative activity assay	GI50 = 1.26 μM	27017549
SK-MEL-28	Antiproliferative activity assay	EC50 = 1.3 μM	18942827
sf9	Function assay	Kd = 1.3 μM	28109791
F-6-8	Cytotoxicity assay	IC50 = 1.3 μM	26318998
A549	Antiproliferative activity assay	IC50 = 1.45 μM	26342134
rhabdomyosarcoma	Antiviral activity assay	EC50 = 1.5 μM	27288186
HL-60(TB)	Growth inhibition assay	GI50 = 1.58 μM	28088086
RPMI8226	Growth inhibition assay	GI50 = 1.58 μM	28088086
KM12	Growth inhibition assay	GI50 = 1.58 μM	28088086
LOXIMVI	Growth inhibition assay	GI50 = 1.58 μM	28088086
HCT116	Growth inhibition assay	GI50 = 1.58 μM	28088086
HOP92	Growth inhibition assay	GI50 = 1.58 μM	28088086
SF539	Growth inhibition assay	GI50 = 1.58 μM	28088086
UACC62	Growth inhibition assay	GI50 = 1.58 μM	28088086
SF295	Growth inhibition assay	GI50 = 1.58 μM	28088086
MDA-MB-435	Growth inhibition assay	GI50 = 1.58 μM	28088086
SK-MEL-5	Growth inhibition assay	GI50 = 1.58 μM	28088086
T47D	Growth inhibition assay	GI50 = 1.58 μM	28088086
RPMI8266	Cytotoxicity assay	GI50 = 1.58 μM	26590508
HL-60(TB)	Cytotoxicity assay	GI50 = 1.58 μM	26590508
KM12	Cytotoxicity assay	GI50 = 1.58 μM	26590508
HCT116	Cytotoxicity assay	GI50 = 1.58 μM	26590508
SF295	Cytotoxicity assay	GI50 = 1.58 μM	26590508
SF539	Cytotoxicity assay	GI50 = 1.58 μM	26590508
SK-MEL-2	Cytotoxicity assay	GI50 = 1.58 μM	26590508
MDA-MB-435	Cytotoxicity assay	GI50 = 1.58 μM	26590508
SK-MEL-5	Cytotoxicity assay	GI50 = 1.58 μM	26590508
LOXIMVI	Cytotoxicity assay	GI50 = 1.58 μM	26590508
T47D	Cytotoxicity assay	GI50 = 1.58 μM	26590508
SMMC7721	Antiproliferative activity assay	IC50 = 1.58 μM	26753815
LOXIMVI	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
UACC62	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
SK-MEL-5	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
KM12	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
MDA-MB-435	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
SF539	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
SF295	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
HCT116	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
HOP92	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
RPMI8226	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
HL-60(TB)	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
T47D	Antiproliferative activity assay	GI50 = 1.58 μM	27017549
7dF3	Function assay	IC50 = 1.62 μM	29266937
MDA-MB-435	Antiproliferative activity assay	IC50 = 1.67 μM	25778995
HL60	Cytotoxicity assay	IC50 = 1.68 μM	24858546
SW579	Antiproliferative activity human	IC50 = 1.73 μM	28242553
MCF7	Antiproliferative activity assay	IC50 = 1.88 μM	25637123
A375P	Antiproliferative activity assay	IC50 = 1.9 μM	24128410
A549	Cytotoxicity assay	IC50 = 1.92 μM	24826815
HCT116	Antiproliferative activity assay	IC50 = 2 μM	22808911
MDA-MB-231	Cytotoxicity assay	IC50 = 2 μM	23454017
NCI-H23	Growth inhibition assay	GI50 = 2 μM	28088086
NCI-H522	Growth inhibition assay	GI50 = 2 μM	28088086
HOP62	Growth inhibition assay	GI50 = 2 μM	28088086
NCI-H226	Growth inhibition assay	GI50 = 2 μM	28088086
HT-29	Growth inhibition assay	GI50 = 2 μM	28088086
U251	Growth inhibition assay	GI50 = 2 μM	28088086
COLO205	Growth inhibition assay	GI50 = 2 μM	28088086
CCRF-CEM	Growth inhibition assay	GI50 = 2 μM	28088086
MALME-3M	Growth inhibition assay	GI50 = 2 μM	28088086
M14	Growth inhibition assay	GI50 = 2 μM	28088086
UACC257	Growth inhibition assay	GI50 = 2 μM	28088086
PC3	Growth inhibition assay	GI50 = 2 μM	28088086
SK-MEL-2	Growth inhibition assay	GI50 = 2 μM	28088086
MDA-MB-468	Growth inhibition assay	GI50 = 2 μM	28088086
CCRF-CEM	Cytotoxicity assay	GI50 = 2 μM	26590508
NCI-H23	Cytotoxicity assay	GI50 = 2 μM	26590508
NCI-H522	Cytotoxicity assay	GI50 = 2 μM	26590508
COLO205	Cytotoxicity assay	GI50 = 2 μM	26590508
HT-29	Cytotoxicity assay	GI50 = 2 μM	26590508
SK-MEL-28	Cytotoxicity assay	GI50 = 2 μM	26590508
HOP62	Cytotoxicity assay	GI50 = 2 μM	26590508
UACC257	Cytotoxicity assay	GI50 = 2 μM	26590508
NCI-H226	Cytotoxicity assay	GI50 = 2 μM	26590508
U251	Cytotoxicity assay	GI50 = 2 μM	26590508
PC3	Cytotoxicity assay	GI50 = 2 μM	26590508
M14	Cytotoxicity assay	GI50 = 2 μM	26590508
MDA-MB-468	Cytotoxicity assay	GI50 = 2 μM	26590508
PC3	Antiproliferative activity assay	GI50 = 2 μM	27017549
MALME-3M	Antiproliferative activity assay	GI50 = 2 μM	27017549
U251	Antiproliferative activity assay	GI50 = 2 μM	27017549
UACC257	Antiproliferative activity assay	GI50 = 2 μM	27017549
SK-MEL-2	Antiproliferative activity assay	GI50 = 2 μM	27017549
COLO205	Antiproliferative activity assay	GI50 = 2 μM	27017549
NCI-H23	Antiproliferative activity assay	GI50 = 2 μM	27017549
HT-29	Antiproliferative activity assay	GI50 = 2 μM	27017549
M14	Antiproliferative activity assay	GI50 = 2 μM	27017549
NCI-H226	Antiproliferative activity assay	GI50 = 2 μM	27017549
HOP62	Antiproliferative activity assay	GI50 = 2 μM	27017549
MDA-MB-468	Antiproliferative activity assay	GI50 = 2 μM	27017549
CCRF-CEM	Antiproliferative activity assay	GI50 = 2 μM	27017549
NCI-H522	Antiproliferative activity assay	GI50 = 2 μM	27017549
A549	Antiproliferative activity assay	IC50 = 2.02 μM	26753815
MDA-MB-435	Growth inhibition assay	IC50 = 2.11 μM	29189002
NCI-H460	Antiproliferative activity assay	IC50 = 2.19 μM	30216849
H460	Cytotoxicity assay	IC50 = 2.19 μM	24826815
H460	Cytotoxicity assay	IC50 = 2.19 μM	25086238
H460	Cytotoxicity assay	IC50 = 2.19 μM	25440879
A375	Toxicity assay	IC50 = 2.2 μM	19654408
H460	Antiproliferative activity assay	IC50 = 2.25 μM	26991938
HCT116	Antiproliferative activity assay	IC50 = 2.3 μM	23260578
MKN45	Antiproliferative activity assay	IC50 = 2.32 μM	30216849
MKN45	Cytotoxicity assay	IC50 = 2.32 μM	24826815
MKN45	Cytotoxicity assay	IC50 = 2.32 μM	25086238
MKN45	Cytotoxicity assay	IC50 = 2.32 μM	25440879
U937	Antiproliferative activity assay	GI50 = 2.34 μM	29459144
A375	Antiproliferative activity assay	IC50 = 2.4 μM	22808911
HeLa	Growth inhibition assay	IC50 = 2.44 μM	29102175
MDA-MB-231	Cytotoxicity assay	IC50 = 2.5 μM	22414612
MCF7	Antiproliferative activity assay	IC50 = 2.51 μM	30216849
UO31	Antiproliferative activity assay	IC50 = 2.51 μM	30216849
NCI-H322M	Growth inhibition assay	GI50 = 2.51 μM	28088086
NCI-H460	Growth inhibition assay	GI50 = 2.51 μM	28088086
KM12	Growth inhibition assay	TGI = 2.51 μM	28088086
LOXIMVI	Growth inhibition assay	TGI = 2.51 μM	28088086
EKVX	Growth inhibition assay	GI50 = 2.51 μM	28088086
HCT116	Growth inhibition assay	TGI = 2.51 μM	28088086
SW620	Growth inhibition assay	GI50 = 2.51 μM	28088086
SF268	Growth inhibition assay	GI50 = 2.51 μM	28088086
SF539	Growth inhibition assay	TGI = 2.51 μM	28088086
A498	Growth inhibition assay	GI50 = 2.51 μM	28088086
UACC62	Growth inhibition assay	TGI = 2.51 μM	28088086
IGROV1	Growth inhibition assay	GI50 = 2.51 μM	28088086
HCT15	Growth inhibition assay	GI50 = 2.51 μM	28088086
SK-MEL-28	Growth inhibition assay	GI50 = 2.51 μM	28088086
SK-MEL-28	Growth inhibition assay	TGI = 2.51 μM	28088086
ACHN	Growth inhibition assay	GI50 = 2.51 μM	28088086
SK-MEL-5	Growth inhibition assay	TGI = 2.51 μM	28088086
NCI/ADR-RES	Growth inhibition assay	GI50 = 2.51 μM	28088086
MCF7	Growth inhibition assay	GI50 = 2.51 μM	28088086
SN12C	Growth inhibition assay	GI50 = 2.51 μM	28088086
Hs 578T	Growth inhibition assay	GI50 = 2.51 μM	28088086
SKOV3	Growth inhibition assay	GI50 = 2.51 μM	28088086
UO31	Growth inhibition assay	GI50 = 2.51 μM	28088086
NCI-H460	Cytotoxicity assay	GI50 = 2.51 μM	26590508
HCT15	Cytotoxicity assay	GI50 = 2.51 μM	26590508
SW620	Cytotoxicity assay	GI50 = 2.51 μM	26590508
SF268	Cytotoxicity assay	GI50 = 2.51 μM	26590508
IGROV1	Cytotoxicity assay	GI50 = 2.51 μM	26590508
OVCAR8	Cytotoxicity assay	GI50 = 2.51 μM	26590508
NCI/ADR-RES	Cytotoxicity assay	GI50 = 2.51 μM	26590508
SKOV3	Cytotoxicity assay	GI50 = 2.51 μM	26590508
SN12C	Cytotoxicity assay	GI50 = 2.51 μM	26590508
NCI-H322M	Cytotoxicity assay	GI50 = 2.51 μM	26590508
MCF7	Cytotoxicity assay	GI50 = 2.51 μM	26590508
UO31	Cytotoxicity assay	GI50 = 2.51 μM	26590508
Hs578T	Cytotoxicity assay	GI50 = 2.51 μM	26590508
A498	Cytotoxicity assay	GI50 = 2.51 μM	26590508
A498	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
SKOV3	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
UO31	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
NCI-ADR-RES	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
SN12C	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
IGROV1	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
ACHN	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
OVCAR8	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
SK-MEL-28	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
NCI-H322M	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
SF268	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
HCT15	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
NCI-H460	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
SW620	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
EKVX	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
MCF7	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
Hs 578T	Antiproliferative activity assay	GI50 = 2.51 μM	27017549
HT-29	Antiproliferative activity assay	IC50 = 2.58 μM	29886324
A375P	Antiproliferative activity assay	GI50 = 2.58 μM	26810260
TPC1	Antiproliferative activity assay	EC50 = 2.6 μM	22559926
Hep3B	Growth inhibition assay	IC50 = 2.63 μM	29102175
A375P	Antiproliferative activity assay	IC50 = 2.7 μM	22460030
U937	Antiproliferative activity assay	GI50 = 2.74 μM	26318067
U937	Cytotoxicity assay	GI50 = 2.74 μM	24878193
MCF7	Growth inhibition assay	IC50 = 2.78 μM	29102175
MDA-MB-231	Antiproliferative activity assay	IC50 = 2.8 μM	29202403
HepG2	Antiproliferative activity assay	IC50 = 2.84 μM	28242553
U937	Growth inhibition assay	GI50 = 2.85 μM	22014755
A549	Cytotoxicity assay	IC50 = 2.92 μM	28927801
A549	Cytotoxicity assay	IC50 = 2.92 μM	27777009
ZR75-30	Growth inhibition assay	IC50 = 2.96 μM	29102175
PC3	Cytotoxicity assay	IC50 = 3.03 μM	28340913
MDA-MB-231	Antiproliferative activity assay	IC50 = 3.08 μM	26991938
A549	Growth inhibition assay	IC50 = 3.1 μM	29102175
K562	Growth inhibition assay	GI50 = 3.16 μM	28088086
MOLT4	Growth inhibition assay	GI50 = 3.16 μM	28088086
A549/ATCC	Growth inhibition assay	GI50 = 3.16 μM	28088086
RPMI8226	Growth inhibition assay	TGI = 3.16 μM	28088086
SR	Growth inhibition assay	GI50 = 3.16 μM	28088086
HOP62	Growth inhibition assay	TGI = 3.16 μM	28088086
NCI-H226	Growth inhibition assay	TGI = 3.16 μM	28088086
U251	Growth inhibition assay	TGI = 3.16 μM	28088086
COLO205	Growth inhibition assay	TGI = 3.16 μM	28088086
M14	Growth inhibition assay	TGI = 3.16 μM	28088086
HCC2998	Growth inhibition assay	GI50 = 3.16 μM	28088086
SNB75	Growth inhibition assay	GI50 = 3.16 μM	28088086
786-0	Growth inhibition assay	GI50 = 3.16 μM	28088086
A498	Growth inhibition assay	TGI = 3.16 μM	28088086
HCT15	Growth inhibition assay	TGI = 3.16 μM	28088086
OVCAR3	Growth inhibition assay	GI50 = 3.16 μM	28088086
OVCAR4	Growth inhibition assay	GI50 = 3.16 μM	28088086
Caki1	Growth inhibition assay	GI50 = 3.16 μM	28088086
SNB19	Growth inhibition assay	GI50 = 3.16 μM	28088086
OVCAR5	Growth inhibition assay	GI50 = 3.16 μM	28088086
DU145	Growth inhibition assay	GI50 = 3.16 μM	28088086
OVCAR8	Growth inhibition assay	GI50 = 3.16 μM	28088086
SN12C	Growth inhibition assay	TGI = 3.16 μM	28088086
MDA-MB-231	Growth inhibition assay	TGI = 3.16 μM	28088086
RXF393	Growth inhibition assay	GI50 = 3.16 μM	28088086
BT549	Growth inhibition assay	GI50 = 3.16 μM	28088086
K562	Cytotoxicity assay	GI50 = 3.16 μM	26590508
MOLT4	Cytotoxicity assay	GI50 = 3.16 μM	26590508
SNB19	Cytotoxicity assay	GI50 = 3.16 μM	26590508
SR	Cytotoxicity assay	GI50 = 3.16 μM	26590508
A549	Cytotoxicity assay	GI50 = 3.16 μM	26590508
OVCAR3	Cytotoxicity assay	GI50 = 3.16 μM	26590508
OVCAR4	Cytotoxicity assay	GI50 = 3.16 μM	26590508
SNB75	Cytotoxicity assay	GI50 = 3.16 μM	26590508
OVCAR5	Cytotoxicity assay	GI50 = 3.16 μM	26590508
DU145	Cytotoxicity assay	GI50 = 3.16 μM	26590508
786-0	Cytotoxicity assay	GI50 = 3.16 μM	26590508
BT549	Cytotoxicity assay	GI50 = 3.16 μM	26590508
ACHN	Cytotoxicity assay	GI50 = 3.16 μM	26590508
Caki1	Cytotoxicity assay	GI50 = 3.16 μM	26590508
786-0	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
LOXIMVI	Antiproliferative activity assay	TGI = 3.16 μM	27017549
Caki1	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
OVCAR5	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
RXF393	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
SNB75	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
OVCAR3	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
SNB19	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
SK-MEL-5	Antiproliferative activity assay	TGI = 3.16 μM	27017549
OVCAR4	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
SK-MEL-2	Antiproliferative activity assay	TGI = 3.16 μM	27017549
BT549	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
MOLT4	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
K562	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
HCC2998	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
HCC2998	Antiproliferative activity assay	TGI = 3.16 μM	27017549
A549/ATCC	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
DU145	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
SR	Antiproliferative activity assay	GI50 = 3.16 μM	27017549
MCF7	Cytotoxicity assay	IC50 = 3.18 μM	28927801
PC3	Cytotoxicity assay	IC50 = 3.18 μM	28927801
MCF7	Cytotoxicity assay	IC50 = 3.18 μM	27777009
A549	Antiproliferative activity assay	IC50 = 3.19 μM	25778995
PC3	Cytotoxicity assay	IC50 = 3.24 μM	27777009
HeLa	Function assay	IC50 = 3.3 μM	15225706
HeLa	Function assay	IC50 = 3.3 μM	15225706
LoVo	Cytotoxicity assay	IC50 = 3.3 μM	23454017
A375	Antiproliferative activity assay	IC50 = 3.36 μM	29602674
HT-29	Antiproliferative activity assay	IC50 = 3.37 μM	26991938
FLT3 gene-deficient U937	Antiproliferative activity assay	GI50 = 3.4 μM	21708468
FLT3 negative U937	Cytotoxicity assay	GI50 = 3.4 μM	23618709
U937	Cytotoxicity assay	GI50 = 3.4 μM	26081023
A375P	Antiproliferative activity assay	GI50 = 3.4 μM	29459144
ACHN	Cytotoxicity assay	IC50 = 3.4 μM	29517908
ACHN	Cytotoxicity assay	IC50 = 3.4 μM	29297688
HepG2	Function assay	IC50 = 3.4 μM	26071861
A375P	Cytotoxicity assay	GI50 = 3.4 μM	24878193
HepG2	Cytotoxicity assay	IC50 = 3.44 μM	28927801
HepG2	Cytotoxicity assay	IC50 = 3.44 μM	27777009
ACHN	Cytotoxicity assay	IC50 = 3.5 μM	29786436
HepG2	Antiproliferative activity assay	IC50 = 3.5 μM	25462265
HT-29	Cytotoxicity assay	IC50 = 3.61 μM	24826815
HT-29	Antiproliferative activity assay	IC50 = 3.61 μM	30216849
HT-29	Cytotoxicity assay	IC50 = 3.61 μM	25086238
HT-29	Cytotoxicity assay	IC50 = 3.61 μM	25440879
MCF7	Anticancer activity assay	IC50 = 3.64 μM	29549841
Sf9	Function assay	IC50 = 3.8 μM	21708468
Sf9	Function assay	IC50 = 3.8 μM	23618709
Sf9	Function assay	IC50 = 3.8 μM	26081023
A2058	Cytotoxicity assay	IC50 = 3.8 μM	22708987
NCI-H460	Cytotoxicity assay	IC50 = 3.9 μM	23454017
SK-MEL-30	Cytotoxicity assay	IC50 = 3.9 μM	29461827
HT-29	Anticancer activity assay	IC50 = 3.97 μM	29549841
SF268	Growth inhibition assay	TGI = 3.98 μM	28088086
SNB75	Growth inhibition assay	TGI = 3.98 μM	28088086
OVCAR3	Growth inhibition assay	TGI = 3.98 μM	28088086
SNB19	Growth inhibition assay	TGI = 3.98 μM	28088086
Hs 578T	Growth inhibition assay	TGI = 3.98 μM	28088086
TK10	Growth inhibition assay	GI50 = 3.98 μM	28088086
BT549	Growth inhibition assay	TGI = 3.98 μM	28088086
Caki1	Antiproliferative activity assay	TGI = 3.98 μM	27017549
TK10	Antiproliferative activity assay	GI50 = 3.98 μM	27017549
MDA-MB-435	Antiproliferative activity assay	TGI = 3.98 μM	27017549
HCT116	Antiproliferative activity assay	TGI = 3.98 μM	27017549
MDA-MB-231	Antiproliferative activity assay	TGI = 3.98 μM	27017549
HepG2	Cytotoxicity assay	IC50 = 4 μM	23454017
HT-29	Cytotoxicity assay	IC50 = 4 μM	23454017
A549	Cytotoxicity assay	IC50 = 4 μM	23454017
HuH7	Cytotoxicity assay	GI50 = 4 μM	23726028
PC3	Antiproliferative activity assay	IC50 = 4.13 μM	25778995
HeLa	Cytotoxicity assay	IC50 = 4.163 μM	23362959
MDA-MB-436	Antiproliferative activity assay	IC50 = 4.2 μM	29202403
MCF7	Cytotoxicity assay	IC50 = 4.21 μM	27043268
MCF7	Cytotoxicity assay	IC50 = 4.21 μM	28340913
LOXIMVI	Antiproliferative activity assay	IC50 = 4.25 μM	25778995
OVCAR4	Cytotoxicity assay	TGI = 4.31 μM	26590508
WM1361	Antiproliferative activity assay	GI50 = 4.345 μM	20148563
WM266.4	Growth inhibition assay	GI50 = 4.5 μM	20199087
HepG2	Cytotoxicity assay	GI50 = 4.5 μM	23726028
A549	Antiproliferative activity assay	IC50 = 4.5 μM	23260578
LS174T	Function assay	IC50 = 4.52 μM	29266937
8505C	Antiproliferative activity assay	IC50 = 4.7 μM	29032031
OVCAR8	Cytotoxicity assay	TGI = 4.73 μM	26590508
MDA-MB-231	Cytotoxicity assay	IC50 = 4.77 μM	20435479
B16-F1	Antiproliferative activity assay	IC50 = 4.9 μM	18477505
WM164	Antiproliferative activity assay	IC50 = 4.9 μM	17561392
B16-F1	Antiproliferative activity assay	IC50 = 4.9 μM	20056548
MDA-MB-468	Cytotoxicity assay	IC50 = 4.9 μM	26159483
786-O	Cytotoxicity assay	IC50 = 4.9 μM	29517908
786-O	Cytotoxicity assay	IC50 = 4.9 μM	29297688
WM266.4	Antiproliferative activity assay	GI50 = 4.933 μM	20148563
WM266.4	Growth inhibition assay	IC50 = 5 μM	19323560
WM164	Antiproliferative activity assay	IC50 = 5 μM	20056548
HepG2	Antiproliferative activity assay	IC50 = 5 μM	23260578
HepG2	Antiproliferative activity assay	IC50 = 5 μM	23932071
NCI-H23	Growth inhibition assay	TGI = 5.01 μM	28088086
NCI-H322M	Growth inhibition assay	TGI = 5.01 μM	28088086
NCI-H460	Growth inhibition assay	TGI = 5.01 μM	28088086
NCI-H522	Growth inhibition assay	TGI = 5.01 μM	28088086
HT-29	Growth inhibition assay	TGI = 5.01 μM	28088086
CCRF-CEM	Growth inhibition assay	TGI = 5.01 μM	28088086
SW620	Growth inhibition assay	TGI = 5.01 μM	28088086
HOP92	Growth inhibition assay	TGI = 5.01 μM	28088086
786-0	Growth inhibition assay	TGI = 5.01 μM	28088086
MDA-MB-435	Growth inhibition assay	TGI = 5.01 μM	28088086
PC3	Growth inhibition assay	TGI = 5.01 μM	28088086
UACC257	Growth inhibition assay	TGI = 5.01 μM	28088086
SKOV3	Growth inhibition assay	TGI = 5.01 μM	28088086
RXF393	Growth inhibition assay	TGI = 5.01 μM	28088086
T47D	Growth inhibition assay	TGI = 5.01 μM	28088086
MDA-MB-468	Growth inhibition assay	TGI = 5.01 μM	28088086
UACC62	Antiproliferative activity assay	TGI = 5.01 μM	27017549
UACC257	Antiproliferative activity assay	TGI = 5.01 μM	27017549
SK-MEL-5	Antiproliferative activity assay	LC50 = 5.01 μM	27017549
M14	Antiproliferative activity assay	TGI = 5.01 μM	27017549
NCI-H23	Antiproliferative activity assay	TGI = 5.01 μM	27017549
SF295	Antiproliferative activity assay	TGI = 5.01 μM	27017549
HOP92	Antiproliferative activity assay	TGI = 5.01 μM	27017549
BT549	Antiproliferative activity assay	TGI = 5.01 μM	27017549
MDA-MB-231	Cytotoxicity assay	IC50 = 5.1 μM	26159483
DU145	Cytotoxicity assay	IC50 = 5.1 μM	22708987
A549	Cytotoxicity assay	IC50 = 5.21 μM	20181414
HeLa	Cytotoxicity assay	IC50 = 5.23 μM	26342867
786-O	Cytotoxicity assay	IC50 = 5.3 μM	29786436
HCT116	Antiproliferative activity assay	GI50 = 5.4 μM	15225706
A375	Antiproliferative activity assay	IC50 = 5.4 μM	18477505
SK-MEL-188	Antiproliferative activity assay	IC50 = 5.4 μM	17561392
A375	Antiproliferative activity assay	IC50 = 5.4 μM	20056548
MCF7	Cytotoxicity assay	IC50 = 5.5 μM	26159483
A375	Antiproliferative activity assay	IC50 = 5.58 μM	19464887
A375P	Cytotoxicity assay	IC50 = 5.58 μM	20797858
A375P	Antiproliferative activity assay	GI50 = 5.58 μM	21353571
A375P	Growth inhibition assay	GI50 = 5.58 μM	22014755
A375P	Growth inhibition assay	GI50 = 5.58 μM	20149658
A375P	Antiproliferative activity assay	GI50 = 5.58 μM	20466542
A375P	Antiproliferative activity assay	IC50 = 5.6 μM	19857963
A375P	Antiproliferative activity assay	IC50 = 5.6 μM	21592628
A375P	Antiproliferative activity assay	IC50 = 5.6 μM	22033063
A375P	Cytotoxicity assay	IC50 = 5.6 μM	19897366
A375P	Antiproliferative activity assay	IC50 = 5.6 μM	22647720
HCT116	Cytotoxicity assay	IC50 = 5.65 μM	24215818
SH-SY5Y	Antiproliferative activity assay	IC50 = 5.73 μM	24315192
HepG2	Cytotoxicity assay	IC50 = 5.74 μM	25461318
Bel7402	Cytotoxicity assay	IC50 = 5.8 μM	23454017
HT-29	Cytotoxicity assay	IC50 = 5.9 μM	28865276
melanoma	Growth inhibition assay	IC50 = 6.1 μM	16392826
K562	Antiproliferative activity assay	GI50 = 6.2 μM	21708468
HepG2	Cytotoxicity assay	IC50 = 6.2 μM	28865276
A549	Anticancer activity assay	IC50 = 6.21 μM	29549841
SMMC7721	Antiproliferative activity assay	IC50 = 6.23 μM	22721924
HepG2	Antiproliferative activity assay	IC50 = 6.3 μM	23932071
SF295	Growth inhibition assay	TGI = 6.31 μM	28088086
SK-MEL-2	Growth inhibition assay	TGI = 6.31 μM	28088086
OVCAR5	Growth inhibition assay	TGI = 6.31 μM	28088086
UO31	Growth inhibition assay	TGI = 6.31 μM	28088086
A498	Antiproliferative activity assay	TGI = 6.31 μM	27017549
MALME-3M	Antiproliferative activity assay	TGI = 6.31 μM	27017549
U251	Antiproliferative activity assay	TGI = 6.31 μM	27017549
SK-MEL-2	Antiproliferative activity assay	LC50 = 6.31 μM	27017549
RPMI8226	Antiproliferative activity assay	TGI = 6.31 μM	27017549
HCC2998	Antiproliferative activity assay	LC50 = 6.31 μM	27017549
NCI-H522	Antiproliferative activity assay	TGI = 6.31 μM	27017549
HUVEC	Antiproliferative activity assay	IC50 = 6.42 μM	23644219
A549	Cytotoxicity assay	IC50 = 6.53 μM	27043268
A549	Cytotoxicity assay	IC50 = 6.53 μM	28340913
LoVo	Antiproliferative activity assay	IC50 = 6.56 μM	24315192
A375	Function assay	IC50 = 6.599 μM	21807507
HCT116	Function assay	GI50 = 6.6 μM	15225706
HepG2	Cytotoxicity assay	IC50 = 6.7 μM	26159483
BCPAP	Antiproliferative activity assay	IC50 = 6.7 μM	29032031
A549	Cytotoxicity assay	IC50 = 6.7 μM	28865276
PC3	Cytotoxicity assay	IC50 = 6.8 μM	23021967
SGC7901	Cytotoxicity assay	IC50 = 6.9 μM	23454017
OS-RC2	Cytotoxicity assay	IC50 = 7 μM	29517908
OS-RC2	Cytotoxicity assay	IC50 = 7 μM	29297688
COLO205	Antiproliferative activity human	IC50 = 7.04 μM	28242553
rhabdomyosarcoma	Cytotoxicity activity against human	CC50 = 7.05 μM	27288186
HuH7	Cytotoxicity assay	IC50 = 7.1 μM	26159483
MDA-MB-231	Antiproliferative activity assay	IC50 = 7.18 μM	22721924
FLT3-negative K562	Cytotoxicity assay	GI50 = 7.3 μM	23618709
K562	Function assay	GI50 = 7.3 μM	26081023
K562	Function assay	GI50 = 7.3 μM	26081023
MCF7	Antiproliferative activity assay	IC50 = 7.33 μM	23644219
A549	Cytotoxicity assay	TGI = 7.36 μM	26590508
WI38	Cytotoxicity assay	IC50 = 7.54 μM	24826815
A375	Cytotoxicity assay	IC50 = 7.56 μM	24215818
MDA-MB-231	Cytotoxicity assay	IC50 = 7.62 μM	20181414
786-0	Cytotoxicity assay	TGI = 7.62 μM	26590508
HS27	Antiproliferative activity assay	IC50 = 7.8 μM	19857963
HS27	Cytotoxicity assay	IC50 = 7.8 μM	19897366
HCT116	Cytotoxicity assay	IC50 = 7.8 μM	22483592
HS27	Antiproliferative activity assay	IC50 = 7.85 μM	19464887
HS27	Antiproliferative activity assay	GI50 = 7.85 μM	21353571
A549/ATCC	Growth inhibition assay	TGI = 7.94 μM	28088086
DU145	Growth inhibition assay	TGI = 7.94 μM	28088086
NCI/ADR-RES	Growth inhibition assay	TGI = 7.94 μM	28088086
MCF7	Growth inhibition assay	TGI = 7.94 μM	28088086
PC3	Antiproliferative activity assay	TGI = 7.94 μM	27017549
UO31	Antiproliferative activity assay	TGI = 7.94 μM	27017549
NCI-ADR-RES	Antiproliferative activity assay	TGI = 7.94 μM	27017549
LOXIMVI	Antiproliferative activity assay	LC50 = 7.94 μM	27017549
SK-MEL-28	Antiproliferative activity assay	TGI = 7.94 μM	27017549
KM12	Antiproliferative activity assay	TGI = 7.94 μM	27017549
COLO205	Antiproliferative activity assay	TGI = 7.94 μM	27017549
HT-29	Antiproliferative activity assay	TGI = 7.94 μM	27017549
NCI-H226	Antiproliferative activity assay	TGI = 7.94 μM	27017549
HOP62	Antiproliferative activity assay	TGI = 7.94 μM	27017549
T47D	Antiproliferative activity assay	TGI = 7.94 μM	27017549
MDA-MB-468	Antiproliferative activity assay	TGI = 7.94 μM	27017549
EKVX	Antiproliferative activity assay	TGI = 7.94 μM	27017549
MCF7	Antiproliferative activity assay	TGI = 7.94 μM	27017549
Hs 578T	Antiproliferative activity assay	TGI = 7.94 μM	27017549
MGC803	Antiproliferative activity assay	IC50 = 7.99 μM	26560049
HCT116	Antiproliferative activity assay	IC50 = 8.08 μM	24440479
PC3	Cytotoxicity assay	IC50 = 8.08 μM	27043268
HCT116	Antiproliferative activity assay	IC50 = 8.08 μM	23644219
WM266.4	Antiproliferative activity assay	GI50 = 8.1 μM	23025996
WM266.4	Antiproliferative activity assay	GI50 = 8.12 μM	22583669
Ketr3	Antiproliferative activity assay	IC50 = 8.27 μM	30216849
A375	Antiproliferative activity assay	IC50 = 8.27 μM	30216849
HepG2	Antiproliferative activity assay	IC50 = 8.27 μM	30216849
MX1	Antiproliferative activity assay	IC50 = 8.27 μM	30216849
MX1	Cytotoxicity assay	IC50 = 8.27 μM	24675135
WM266.4	Growth inhibition assay	GI50 = 8.3 μM	22361686
PLC/PRF/5	Cytotoxicity assay	IC50 = 8.3 μM	21531053
A375	Antiproliferative activity assay	IC50 = 8.33 μM	29886324
HCT116	Cytotoxicity assay	IC50 = 8.41 μM	29631788
WI38	Cytotoxicity assay	IC50 = 8.42 μM	26991938
HepG2	Cytotoxicity assay	IC50 = 8.42 μM	27162123
HepG2	Cytotoxicity assay	IC50 = 8.42 μM	23871909
HT-29	Antiproliferative activity assay	IC50 = 8.44 μM	29602674
HepG2	Cytotoxicity assay	IC50 = 8.67 μM	24675135
MCF7	Cytotoxicity assay	IC50 = 8.83 μM	20435479
MCF7	Cytotoxicity assay	IC50 = 9.12 μM	24300920
HepG2	Antiproliferative activity assay	IC50 = 9.14 μM	26560049
A375	Cytotoxicity assay	IC50 = 9.17 μM	24675135
MGC803	Antiproliferative activity assay	IC50 = 9.2 μM	29032031
SKOV3	Cytotoxicity assay	IC50 = 9.25 μM	24300920
RS4:11	Function assay	GI50 = 9.3 μM	26081023
RS4:11	Cytotoxicity assay	GI50 = 9.3 μM	23618709
MIAPaCa2	Antiproliferative activity assay	IC50 = 9.32 μM	29032031
PANC1	Growth inhibition assay	IC50 = 9.32 μM	29102175
MHCC97H	Growth inhibition assay	IC50 = 9.32 μM	29102175
RS4:11	Antiproliferative activity assay	GI50 = 9.4 μM	21708468
Hep3B	Cytotoxicity assay	IC50 = 9.4 μM	28865276
LoVo	Growth inhibition assay	IC50 = 9.47 μM	29102175
SMMC7721	Antiproliferative activity assay	IC50 = 9.96 μM	25637123
MCF7	Cytotoxicity assay	TGI = 9.97 μM	26590508
IGROV1	Growth inhibition assay	TGI = 10 μM	28088086
ACHN	Growth inhibition assay	TGI = 10 μM	28088086
TK10	Growth inhibition assay	TGI = 10 μM	28088086
786-0	Antiproliferative activity assay	TGI = 10 μM	27017549
SN12C	Antiproliferative activity assay	TGI = 10 μM	27017549
Caki1	Antiproliferative activity assay	LC50 = 10 μM	27017549
TK10	Antiproliferative activity assay	TGI = 10 μM	27017549
RXF393	Antiproliferative activity assay	TGI = 10 μM	27017549
OVCAR8	Antiproliferative activity assay	TGI = 10 μM	27017549
SNB75	Antiproliferative activity assay	TGI = 10 μM	27017549
NCI-H322M	Antiproliferative activity assay	TGI = 10 μM	27017549
MDA-MB-435	Antiproliferative activity assay	LC50 = 10 μM	27017549
SF539	Antiproliferative activity assay	TGI = 10 μM	27017549
SF268	Antiproliferative activity assay	TGI = 10 μM	27017549
NCI-H460	Antiproliferative activity assay	TGI = 10 μM	27017549
DU145	Antiproliferative activity assay	TGI = 10 μM	27017549
K1	Antiproliferative activity assay	IC50 = 10.2 μM	29032031
Bel7402	Cytotoxicity assay	IC50 = 10.26 μM	21504204
Bel7402	Growth inhibition assay	IC50 = 10.31 μM	29102175
OVCAR3	Cytotoxicity assay	TGI = 10.32 μM	26590508
SGC7901	Cytotoxicity assay	IC50 = 10.37 μM	20435479
SNB75	Cytotoxicity assay	TGI = 10.42 μM	26590508
A431	Antiproliferative activity assay	IC50 = 10.46 μM	29032031
SMMC7721	Antiproliferative activity assay	IC50 = 10.61 μM	29032031
GES-1	Cytotoxicity assay	IC50 = 10.68 μM	27162123
H460	Cytotoxicity assay	IC50 = 10.8 μM	24300920
BGC823	Antiproliferative activity assay	IC50 = 10.91 μM	22721924
Hep3B	Cytotoxicity assay	IC50 = 11.2 μM	28342400
MCF7	Cytotoxicity assay	IC50 = 11.34 μM	27162123
MCF7	Cytotoxicity assay	IC50 = 11.34 μM	23871909
SK-MEL-2	Antiproliferative activity human	IC50 = 11.35 μM	28242553
HepG2	Cytotoxicity assay	IC50 = 11.49 μM	21504204
A375P	Antiproliferative activity assay	IC50 = 11.5 μM	22014559
SGC7901	Cytotoxicity assay	IC50 = 11.5 μM	24300920
HeLa	Antiproliferative activity assay	IC50 = 12.01 μM	29103873
PANC1	Cytotoxicity assay	IC50 = 12.3 μM	24300920
HepG2	Antiproliferative activity assay	IC50 = 12.54 μM	29032031
A549	Antiproliferative activity assay	IC50 = 12.54 μM	23644219
Caki1	Growth inhibition assay	TGI = 12.59 μM	28088086
OVCAR8	Growth inhibition assay	TGI = 12.59 μM	28088086
SKOV3	Antiproliferative activity assay	TGI = 12.6 μM	27017549
ACHN	Antiproliferative activity assay	TGI = 12.6 μM	27017549
OVCAR3	Antiproliferative activity assay	TGI = 12.6 μM	27017549
OVCAR4	Antiproliferative activity assay	TGI = 12.6 μM	27017549
HCT15	Antiproliferative activity assay	TGI = 12.6 μM	27017549
SW620	Antiproliferative activity assay	TGI = 12.6 μM	27017549
A549/ATCC	Antiproliferative activity assay	TGI = 12.6 μM	27017549
MDA-MB-468	Cytotoxicity assay	TGI = 13.09 μM	26590508
SK-MEL-28	Cytotoxicity assay	TGI = 13.39 μM	26590508
A549	Antiproliferative activity assay	IC50 = 13.64 μM	26560049
A375	Antiproliferative activity human	IC50 = 13.64 μM	28242553
A375	Antiproliferative activity assay	IC50 = 13.64 μM	25462267
K562	Antiproliferative activity assay	IC50 = 13.85 μM	23644219
Hep3B	Cytotoxicity assay	IC50 = 14.08 μM	21504204
T47D	Cytotoxicity assay	TGI = 14.38 μM	26590508
NCI-H226	Cytotoxicity assay	TGI = 14.42 μM	26590508
MDA-MB-231	Antiproliferative activity assay	IC50 = 14.62 μM	24440479
MDA-MB-231	Antiproliferative activity assay	IC50 = 14.62 μM	23644219
NCI-H522	Cytotoxicity assay	TGI = 14.82 μM	26590508
SK-MEL-2	Cytotoxicity assay	TGI = 14.85 μM	26590508
OS-RC2	Cytotoxicity assay	IC50 = 15 μM	29786436
HepG2	Antiproliferative activity assay	IC50 = 15 μM	29103873
fibroblast	Antiproliferative activity assay	IC50 = 15.1 μM	18477505
HT-29	Cytotoxicity assay	IC50 = 15.2 μM	24675135
U87MG	Cytotoxicity assay	IC50 = 15.57 μM	24826815
BT549	Antiproliferative activity assay	LC50 = 15.8 μM	27017549
GES-1	Cytotoxicity assay	IC50 = 15.8 μM	23871909
SNB19	Antiproliferative activity assay	TGI = 15.85 μM	27017549
IGROV1	Antiproliferative activity assay	TGI = 15.9 μM	27017549
HCT116	Antiproliferative activity assay	LC50 = 15.9 μM	27017549
OS-RC2	Cytotoxicity assay	IC50 = 16 μM	23454017
A375	Cytotoxicity assay	IC50 = 16.24 μM	25461318
SKOV3	Cytotoxicity assay	TGI = 16.36 μM	26590508
WM1361	Antiproliferative activity assay	IC50 = 16.44 μM	29602674
MKN28	Antiproliferative activity assay	IC50 = 17 μM	29032031
SMMC7721	Cytotoxicity assay	IC50 = 17.3 μM	21504204
UACC257	Cytotoxicity assay	TGI = 17.33 μM	26590508
EAhy926	Antiangiogenic activity assay	IC50 = 18.52 μM	29032031
SMMC7721	Cytotoxicity assay	IC50 = 18.7 μM	24300920
Ketr3	Cytotoxicity assay	IC50 = 18.8 μM	24675135
NCI-H522	Cytotoxicity assay	IC50 = 19.26 μM	25461318
A549	Cytotoxicity assay	IC50 = 19.54 μM	27162123
SH-SY5Y	Cytotoxicity assay	IC50 = 19.54 μM	23871909
MGC803	Antiproliferative activity assay	IC50 = 19.92 μM	29103873
EKVX	Growth inhibition assay	TGI = 19.95 μM	28088086
OVCAR5	Antiproliferative activity assay	TGI = 20 μM	27017549
UACC62	Antiproliferative activity assay	LC50 = 20 μM	27017549
UACC257	Antiproliferative activity assay	LC50 = 20 μM	27017549
MDA-MB-231	Antiproliferative activity assay	LC50 = 20 μM	27017549
U87	Cytotoxicity assay	IC50 = 21.07 μM	20435479
EJ	Cytotoxicity assay	IC50 = 22.9 μM	24300920
HCT116	Antiproliferative activity assay	IC50 = 23.31 μM	29602674
HOP62	Cytotoxicity assay	TGI = 23.55 μM	26590508
MDA-MB-231	Cytotoxicity assay	TGI = 23.93 μM	26590508
PC3	Antiproliferative activity assay	IC50 = 24.2 μM	24440479
PC3	Antiproliferative activity assay	IC50 = 24.2 μM	23644219
EAhy926	Antiproliferative activity assay	IC50 = 24.36 μM	28068599
EAhy926	Anti-angiogenic activity in human	IC50 = 24.36 μM	29102175
U251	Cytotoxicity assay	IC50 = 24.71 μM	20435479
NIH/3T3	Antiproliferative activity assay	IC50 = 24.75 μM	21592628
NIH/3T3	Antiproliferative activity assay	IC50 = 24.75 μM	22647720
DU145	Cytotoxicity assay	IC50 = 24.91 μM	27162123
DU145	Cytotoxicity assay	IC50 = 24.91 μM	23871909
U251	Antiproliferative activity assay	LC50 = 25.1 μM	27017549
M14	Antiproliferative activity assay	LC50 = 25.1 μM	27017549
NCI-H522	Antiproliferative activity assay	LC50 = 25.1 μM	27017549
OVCAR4	Growth inhibition assay	TGI = 25.12 μM	28088086
SH-SY5Y	Cytotoxicity assay	IC50 = 27.71 μM	27162123
A549	Cytotoxicity assay	IC50 = 27.71 μM	23871909
PLC/PRF/5	Cytotoxicity assay	IC50 = 29.9 μM	28109948
SK-MEL-5	Cytotoxicity assay	TGI = 31.26 μM	26590508
A498	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
SK-MEL-28	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
KM12	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
COLO205	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
NCI-H226	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
SF295	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
HOP62	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
T47D	Antiproliferative activity assay	LC50 = 31.6 μM	27017549
MHCC97L	Cytotoxicity assay	IC50 = 34.41 μM	28109948
MDA-MB-231	Antiproliferative activity assay	IC50 = 35 μM	24315192
MDA-MB-231	Cytotoxicity assay	IC50 = 36 μM	22483592
B16-BL6	Cytotoxicity assay	IC50 = 36.48 μM	29631788
UO31	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
SN12C	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
RXF393	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
SNB75	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
SF268	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
NCI-H23	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
HT-29	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
HOP92	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
NCI-H460	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
SW620	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
MDA-MB-468	Antiproliferative activity assay	LC50 = 39.8 μM	27017549
MALME-3M	Growth inhibition assay	TGI = 39.81 μM	28088086
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	464.82	Formula	C₂₁H₁₆ClF₃N₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	284461-73-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC-724772,BAY 43-9006			Smiles	CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (197.92 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.76mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 45%PEG400 2 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.380mg/ml (0.82mM)	Taking the 1 mL working solution as an example, add 50 μL of 7.5 mg/ml clarified DMSO stock solution to 450 μL of PEG 400, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (5.38mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Raf-1 (Cell-free assay) 6 nM mVEGFR2(Flk1) (Cell-free assay) 15 nM mVEGFR3 (Cell-free assay) 20 nM B-Raf (Cell-free assay) 22 nM B-Raf (V599E) (Cell-free assay) 38 nM mPDGFRβ (Cell-free assay) 57 nM FLT3 (Cell-free assay) 58 nM c-Kit (Cell-free assay) 68 nM VEGFR2 (Cell-free assay) 90 nM FGFR1 (Cell-free assay) 580 nM
In vitro	Sorafenib inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. This compound also potently inhibits mVEGFR2 (Flk-1), mVEGFR3, mPDGFRβ, Flt3, and c-Kit with IC50 of 15 nM, 20 nM, 57 nM, 58 nM, and 68 nM, respectively. It weakly inhibits FGFR-1 with IC50 of 580 nM. This chemical is not active against ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ, and pim-1. It markedly inhibits VEGFR2 phosphorylation in NIH 3T3 cells with IC50 of 30 nM, and Flt-3 phosphorylation in HEK-293 cells with IC50 of 20 nM. This agent potently blocks MEK 1/2 and ERK 1/2 phosphorylation in most cell lines but not in A549 or H460 cells, while having no effect on inhibition of the PKB pathway. It inhibits the proliferation of HAoSMC and MDA-MB-231 cells with IC50 of 0.28 μM and 2.6 μM, respectively. In addition to inhibition of the RAF/MEK/ERK signaling pathway, this compound significantly inhibits the phosphorylation of eIF4E and down-regulates Mcl-1 levels in hepatocellular carcinoma (HCC) cells in a MEK/ERK-independent manner. It inhibits the proliferation of PLC/PRF/5 and HepG2 cells with IC50 of 6.3 μM and 4.5 μM, respectively, and leads to the significant induction of apoptosis.
Kinase Assay	Biochemical assays
Kinase Assay	Recombinant baculoviruses expressing Raf-1 (residues 305–648) and B-Raf (residues 409–765) are purified as fusion proteins. Full-length human MEK-1 is generated by PCR and purified as a fusion protein from Escherichia coli lysates. Sorafenib tosylate is added to a mixture of Raf-1 (80 ng), or B-Raf (80 ng) with MEK-1 (1 μg) in assay buffer [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl₂, and 0.15% β-mercaptoethanol] at a final concentration of 1% DMSO. The Raf kinase assay (final volume of 50 μL) is initiated by adding 25 μL of 10 μM γ[³³P]ATP (400 Ci/mol) and incubated at 32 °C for 25 minutes. Phosphorylated MEK-1 is harvested by filtration onto a phosphocellulose mat, and 1% phosphoric acid is used to wash away unbound radioactivity. After drying by microwave heating, a β-plate counter is used to quantify filter-bound radioactivity. Human VEGFR2 (KDR) kinase domain is expressed and purified from Sf9 lysates. Time-resolved fluorescence energy transfer assays for VEGFR2 are performed in 96-well opaque plates in the time-resolved fluorescence energy transfer format. Final reaction conditions are as follows: 1 to 10 μM ATP, 25 nM poly GT-biotin, 2 nM Europium-labelled phospho (p)-Tyr antibody (PY20), 10 nM APC, 1 to 7 nM cytoplasmic kinase domain in final concentrations of 1% DMSO, 50 mM HEPES (pH 7.5), 10 mM MgCl₂, 0.1 mM EDTA, 0.015% Brij-35, 0.1 mg/mL BSA, and 0.1% β-mercaptoethanol. Reaction volumes are 100 μL and are initiated by addition of enzyme. Plates are read at both 615 and 665 nM on a Perkin-Elmer VictorV Multilabel counter at ~1.5 to 2.0 hours after reaction initiation. Signal is calculated as a ratio: (665 nm/615 nM) × 10,000 for each well. For IC50 generation, this compound is added before the enzyme initiation. A 50-fold stock plate is made with this compound serially diluted 1:3 in a 50% DMSO/50% distilled water solution. Final concentrations of this chemical range from 10 μM to 4.56 nM in 1% DMSO.
In vivo	Oral administration of Sorafenib (~60 mg/kg) demonstrates broad spectrum, dose-dependent anti-tumor activity against a variety of human tumour xenograft models including MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460, and A549, with no evidence of toxicity. In association with the anti-tumour efficacy, this compound treatment potently inhibits MEK 1/2 phosphorylation and pERK 1/2 levels in HT-29 and MDA-MB-231 xenografts but not in Colo-205 xenografts, and significantly suppresses tumour microvessel area (MVA) and microvessel density (MVD) in MDA MB-231, HT-29 and Colo-205 tumour xenografts. This agent produces dose-dependent growth inhibition of PLC/PRF/5 tumour xenografts in SCID mice with TGIs of 49% and 78% at 10 mg/kg and 30 mg/kg, respectively, consistent with the inhibition of ERK and eIF4E phosphorylation, reduction of the microvessel area, and induction of tumour cell apoptosis. It sensitizes bax^-/- cells to TRAIL in a dose-dependent manner, through a mechanism involving down-regulating NF-κB mediated Mcl-1 and cIAP2 expression. Combining this compound (30-60 mg/kg) with TRAIL (5 mg/kg) show dramatic efficacy in TRAIL-resistant HCT116 bax^-/- and HT29 tumour xenografts.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15466206/ [2] https://pubmed.ncbi.nlm.nih.gov/17178882/ [3] https://pubmed.ncbi.nlm.nih.gov/17613437/

Applications

Methods	Biomarkers	PMID
Western blot	LC3-I / LC-3II / ATG5 p-STAT3 / STAT3 / Mcl-1 β-catenin / Survivin / Mcl-1 / PTMA pERK / ERK p-PKM2(y105) / PMK2 / Caspase-9 RET(pY1016) / VEGFR2(pY1214) / MEK1(pT292) / ERK(pY204) Cyclin D1	23392173
Growth inhibition assay	Cell viability	26039995
Immunofluorescence	p65 cytochrome c	22286758
ELISA	TGF-beta / CD206 Caspase-9 / Caspase-3	26158762

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05068752	Recruiting	Pancreas Cancer	HonorHealth Research Institute\|Bayer\|Genentech Inc.	October 28 2021	Phase 2
NCT04763408	Active not recruiting	Carcinoma Hepatocellular	Eisai Inc.	April 9 2021	--

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