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PLX-4720 B-Raf Inhibitor

Name: PLX-4720
Brand: Selleck Chemicals
SKU: S1152
Rating: 5 (197 reviews)

Cat.No.S1152

PLX4720 is a potent and selective inhibitor of B-Raf^V600E with an IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1 (Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.

Chemical Structure

Molecular Weight: 413.83

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Quality Control

Batch: Purity: 99.98%

99.98

Products Often Used Together with PLX-4720

Dactolisib (BEZ235)

Treatment with this compound and Dactolisib decreases both pERK and pAKT levels in Colo-205 xenografts.

Navitoclax (ABT-263)

It and Navitoclax can enhance the clinical efficacy of BRAF inhibitors.

NMS-E973

It and NMS-E973 show a synergic antiproliferative activity in A375 melanoma cells.

SB431542

Cotreatment with this compound and SB431542 abolish the increase in cell growth caused by low-dose PLX-4720 in Colo829 and A375(M2) cells.

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) AZ 628 SB590885 TAK-632 GW5074 RAF265 (CHIR-265) PLX8394 (Plixorafenib, FORE8394)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
DU-4475	Growth Inhibition Assay		IC50=0.07457 μM	SANGER
EoL-1-cell	Growth Inhibition Assay		IC50=0.14166 μM	SANGER
C32	Growth Inhibition Assay		IC50=0.15131 μM	SANGER
M14	Growth Inhibition Assay		IC50=0.21757 μM	SANGER
CP50-MEL-B	Growth Inhibition Assay		IC50=0.29784 μM	SANGER
A101D	Growth Inhibition Assay		IC50=0.32589 μM	SANGER
G-361	Growth Inhibition Assay		IC50=0.34637 μM	SANGER
HT-144	Growth Inhibition Assay		IC50=0.36329 μM	SANGER
ACN	Growth Inhibition Assay		IC50=0.38477 μM	SANGER
COLO-829	Growth Inhibition Assay		IC50=0.38968 μM	SANGER
MEL-HO	Growth Inhibition Assay		IC50=0.41179 μM	SANGER
SH-4	Growth Inhibition Assay		IC50=0.41422 μM	SANGER
SK-MEL-3	Growth Inhibition Assay		IC50=0.51568 μM	SANGER
A375	Growth Inhibition Assay		IC50=0.67359 μM	SANGER
MMAC-SF	Growth Inhibition Assay		IC50=0.68614 μM	SANGER
BHT-101	Growth Inhibition Assay		IC50=0.70702 μM	SANGER
K5	Growth Inhibition Assay		IC50=0.76148 μM	SANGER
BV-173	Growth Inhibition Assay		IC50=0.79644 μM	SANGER
RVH-421	Growth Inhibition Assay		IC50=0.86796 μM	SANGER
HCC2218	Growth Inhibition Assay		IC50=0.87844 μM	SANGER
WM-115	Growth Inhibition Assay		IC50=0.88692 μM	SANGER
SK-MEL-28	Growth Inhibition Assay		IC50=1.04569 μM	SANGER
COLO-679	Growth Inhibition Assay		IC50=1.10464 μM	SANGER
MZ7-mel	Growth Inhibition Assay		IC50=1.14963 μM	SANGER
SK-MEL-30	Growth Inhibition Assay		IC50=1.33386 μM	SANGER
NCI-H209	Growth Inhibition Assay		IC50=1.6086 μM	SANGER
HTC-C3	Growth Inhibition Assay		IC50=1.66294 μM	SANGER
KARPAS-45	Growth Inhibition Assay		IC50=2.04978 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay		IC50=2.11969 μM	SANGER
KP-4	Growth Inhibition Assay		IC50=2.30787 μM	SANGER
PA-1	Growth Inhibition Assay		IC50=2.72673 μM	SANGER
HuO-3N1	Growth Inhibition Assay		IC50=2.87946 μM	SANGER
NCI-H358	Growth Inhibition Assay		IC50=2.92232 μM	SANGER
CTB-1	Growth Inhibition Assay		IC50=3.40176 μM	SANGER
697	Growth Inhibition Assay		IC50=3.55266 μM	SANGER
CP66-MEL	Growth Inhibition Assay		IC50=4.15927 μM	SANGER
NB13	Growth Inhibition Assay		IC50=4.49179 μM	SANGER
DBTRG-05MG	Growth Inhibition Assay		IC50=4.53325 μM	SANGER
A2058	Growth Inhibition Assay		IC50=4.72164 μM	SANGER
KG-1	Growth Inhibition Assay		IC50=4.73908 μM	SANGER
8305C	Growth Inhibition Assay		IC50=5.1873 μM	SANGER
RPMI-7951	Growth Inhibition Assay		IC50=5.80283 μM	SANGER
CHL-1	Growth Inhibition Assay		IC50=5.97603 μM	SANGER
TI-73	Growth Inhibition Assay		IC50=6.00902 μM	SANGER
HT-1080	Growth Inhibition Assay		IC50=6.10946 μM	SANGER
ES5	Growth Inhibition Assay		IC50=6.14924 μM	SANGER
8-MG-BA	Growth Inhibition Assay		IC50=6.18129 μM	SANGER
NB7	Growth Inhibition Assay		IC50=6.21373 μM	SANGER
H4	Growth Inhibition Assay		IC50=6.22493 μM	SANGER
CAL-72	Growth Inhibition Assay		IC50=6.45423 μM	SANGER
HCC1806	Growth Inhibition Assay		IC50=6.81931 μM	SANGER
BCPAP	Growth Inhibition Assay		IC50=7.21764 μM	SANGER
LB2241-RCC	Growth Inhibition Assay		IC50=7.36907 μM	SANGER
COLO-741	Growth Inhibition Assay		IC50=8.01679 μM	SANGER
HSC-3	Growth Inhibition Assay		IC50=8.07068 μM	SANGER
SW982	Growth Inhibition Assay		IC50=8.41516 μM	SANGER
GCT	Growth Inhibition Assay		IC50=8.75314 μM	SANGER
KY821	Growth Inhibition Assay		IC50=9.05178 μM	SANGER
JVM-3	Growth Inhibition Assay		IC50=9.56999 μM	SANGER
RS4-11	Growth Inhibition Assay		IC50=9.6048 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay		IC50=10.0149 μM	SANGER
A431	Growth Inhibition Assay		IC50=10.4212 μM	SANGER
LXF-289	Growth Inhibition Assay		IC50=10.458 μM	SANGER
SK-MEL-24	Growth Inhibition Assay		IC50=10.8274 μM	SANGER
NOS-1	Growth Inhibition Assay		IC50=10.8472 μM	SANGER
KNS-62	Growth Inhibition Assay		IC50=11.2404 μM	SANGER
SK-HEP-1	Growth Inhibition Assay		IC50=11.3527 μM	SANGER
A3-KAW	Growth Inhibition Assay		IC50=11.7178 μM	SANGER
SK-LU-1	Growth Inhibition Assay		IC50=12.2655 μM	SANGER
TYK-nu	Growth Inhibition Assay		IC50=12.3932 μM	SANGER
NMC-G1	Growth Inhibition Assay		IC50=12.6062 μM	SANGER
BB65-RCC	Growth Inhibition Assay		IC50=12.7169 μM	SANGER
QIMR-WIL	Growth Inhibition Assay		IC50=12.8833 μM	SANGER
D-566MG	Growth Inhibition Assay		IC50=13.9576 μM	SANGER
KYSE-140	Growth Inhibition Assay		IC50=14.0753 μM	SANGER
SCC-4	Growth Inhibition Assay		IC50=14.3359 μM	SANGER
U251	Growth Inhibition Assay		IC50=14.8492 μM	SANGER
D-542MG	Growth Inhibition Assay		IC50=14.9222 μM	SANGER
LAMA-84	Growth Inhibition Assay		IC50=14.9932 μM	SANGER
NCI-H720	Growth Inhibition Assay		IC50=15.2684 μM	SANGER
DEL	Growth Inhibition Assay		IC50=15.4293 μM	SANGER
SBC-1	Growth Inhibition Assay		IC50=15.4305 μM	SANGER
ECC10	Growth Inhibition Assay		IC50=15.4458 μM	SANGER
Daoy	Growth Inhibition Assay		IC50=15.7616 μM	SANGER
SCH	Growth Inhibition Assay		IC50=15.7835 μM	SANGER
MZ2-MEL	Growth Inhibition Assay		IC50=16.0646 μM	SANGER
CAL-12T	Growth Inhibition Assay		IC50=16.4862 μM	SANGER
KE-37	Growth Inhibition Assay		IC50=16.8107 μM	SANGER
LS-411N	Growth Inhibition Assay		IC50=17.118 μM	SANGER
NCI-H2228	Growth Inhibition Assay		IC50=17.3071 μM	SANGER
SK-MEL-2	Growth Inhibition Assay		IC50=17.4965 μM	SANGER
HN	Growth Inhibition Assay		IC50=17.7248 μM	SANGER
NCI-H1648	Growth Inhibition Assay		IC50=17.818 μM	SANGER
IA-LM	Growth Inhibition Assay		IC50=18.3172 μM	SANGER
EW-13	Growth Inhibition Assay		IC50=18.5708 μM	SANGER
YKG-1	Growth Inhibition Assay		IC50=19.5711 μM	SANGER
KNS-81-FD	Growth Inhibition Assay		IC50=19.5858 μM	SANGER
23132-87	Growth Inhibition Assay		IC50=19.7642 μM	SANGER
NUGC-3	Growth Inhibition Assay		IC50=19.9887 μM	SANGER
5637	Growth Inhibition Assay		IC50=20.0478 μM	SANGER
NCI-H1755	Growth Inhibition Assay		IC50=20.4764 μM	SANGER
RH-18	Growth Inhibition Assay		IC50=20.5748 μM	SANGER
RXF393	Growth Inhibition Assay		IC50=20.6756 μM	SANGER
LU-134-A	Growth Inhibition Assay		IC50=20.7056 μM	SANGER
TE-12	Growth Inhibition Assay		IC50=20.7201 μM	SANGER
MOLT-4	Growth Inhibition Assay		IC50=21.1915 μM	SANGER
IGR-1	Growth Inhibition Assay		IC50=21.3796 μM	SANGER
HOP-92	Growth Inhibition Assay		IC50=21.4987 μM	SANGER
SK-MES-1	Growth Inhibition Assay		IC50=21.7381 μM	SANGER
LU-65	Growth Inhibition Assay		IC50=21.8624 μM	SANGER
MS-1	Growth Inhibition Assay		IC50=22.1203 μM	SANGER
LoVo	Growth Inhibition Assay		IC50=22.244 μM	SANGER
A704	Growth Inhibition Assay		IC50=22.5155 μM	SANGER
HT-1376	Growth Inhibition Assay		IC50=22.6059 μM	SANGER
IST-MEL1	Growth Inhibition Assay		IC50=22.6751 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay		IC50=22.7366 μM	SANGER
T47D	Growth Inhibition Assay		IC50=22.7979 μM	SANGER
HT-1197	Growth Inhibition Assay		IC50=23.0817 μM	SANGER
LB2518-MEL	Growth Inhibition Assay		IC50=23.6412 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay		IC50=24.7595 μM	SANGER
SK-NEP-1	Growth Inhibition Assay		IC50=24.8744 μM	SANGER
NCI-H526	Growth Inhibition Assay		IC50=25.0023 μM	SANGER
IST-SL1	Growth Inhibition Assay		IC50=25.2751 μM	SANGER
HH	Growth Inhibition Assay		IC50=25.3192 μM	SANGER
NCI-H82	Growth Inhibition Assay		IC50=25.938 μM	SANGER
SNU-449	Growth Inhibition Assay		IC50=27.2018 μM	SANGER
COR-L23	Growth Inhibition Assay		IC50=27.2813 μM	SANGER
LOXIMVI	Growth Inhibition Assay		IC50=27.368 μM	SANGER
GR-ST	Growth Inhibition Assay		IC50=27.6706 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay		IC50=27.944 μM	SANGER
ALL-PO	Growth Inhibition Assay		IC50=28.1604 μM	SANGER
ML-2	Growth Inhibition Assay		IC50=28.2814 μM	SANGER
HOP-62	Growth Inhibition Assay		IC50=28.713 μM	SANGER
EGI-1	Growth Inhibition Assay		IC50=28.8845 μM	SANGER
TCCSUP	Growth Inhibition Assay		IC50=28.9272 μM	SANGER
LB996-RCC	Growth Inhibition Assay		IC50=29.5682 μM	SANGER
LCLC-97TM1	Growth Inhibition Assay		IC50=32.1964 μM	SANGER
NCI-H1304	Growth Inhibition Assay		IC50=32.3301 μM	SANGER
KP-N-YS	Growth Inhibition Assay		IC50=32.5973 μM	SANGER
NCI-H1770	Growth Inhibition Assay		IC50=33.1648 μM	SANGER
EM-2	Growth Inhibition Assay		IC50=33.6504 μM	SANGER
ChaGo-K-1	Growth Inhibition Assay		IC50=33.7236 μM	SANGER
ACHN	Growth Inhibition Assay		IC50=33.8385 μM	SANGER
MN-60	Growth Inhibition Assay		IC50=33.8544 μM	SANGER
EW-18	Growth Inhibition Assay		IC50=33.8971 μM	SANGER
KGN	Growth Inhibition Assay		IC50=35.7292 μM	SANGER
U031	Growth Inhibition Assay		IC50=35.8132 μM	SANGER
HMV-II	Growth Inhibition Assay		IC50=36.0774 μM	SANGER
L-363	Growth Inhibition Assay		IC50=37.6455 μM	SANGER
NCI-H1155	Growth Inhibition Assay		IC50=38.0015 μM	SANGER
NCI-H1793	Growth Inhibition Assay		IC50=38.1026 μM	SANGER
P30-OHK	Growth Inhibition Assay		IC50=38.1332 μM	SANGER
AN3-CA	Growth Inhibition Assay		IC50=38.1615 μM	SANGER
UACC-257	Growth Inhibition Assay		IC50=38.79 μM	SANGER
MCF7	Growth Inhibition Assay		IC50=39.8629 μM	SANGER
KP-N-YN	Growth Inhibition Assay		IC50=40.4285 μM	SANGER
T98G	Growth Inhibition Assay		IC50=40.4957 μM	SANGER
HGC-27	Growth Inhibition Assay		IC50=43.274 μM	SANGER
NCI-H1092	Growth Inhibition Assay		IC50=43.2895 μM	SANGER
KARPAS-299	Growth Inhibition Assay		IC50=43.3071 μM	SANGER
LB1047-RCC	Growth Inhibition Assay		IC50=44.9959 μM	SANGER
786-0	Growth Inhibition Assay		IC50=45.65 μM	SANGER
HCC2157	Growth Inhibition Assay		IC50=46.0359 μM	SANGER
NY	Growth Inhibition Assay		IC50=46.1778 μM	SANGER
EFM-19	Growth Inhibition Assay		IC50=46.7533 μM	SANGER
EW-16	Growth Inhibition Assay		IC50=46.7806 μM	SANGER
UM-UC-3	Growth Inhibition Assay		IC50=46.8059 μM	SANGER
HT-29	Growth Inhibition Assay		IC50=47.8792 μM	SANGER
LN-405	Growth Inhibition Assay		IC50=48.0827 μM	SANGER
NCI-H727	Growth Inhibition Assay		IC50=48.7726 μM	SANGER
D-502MG	Growth Inhibition Assay		IC50=48.9676 μM	SANGER
GMS-10	Growth Inhibition Assay		IC50=49.2974 μM	SANGER
MEL-JUSO	Growth Inhibition Assay		IC50=49.347 μM	SANGER
insect cells	Function assay		Inhibition of N-terminal His-tagged BRAF V600E mutant (unknown origin) expressed in baculovirus infected insect cells co-expressing CDC37 using biotinylated-MEK as substrate by AlphaScreen assay, IC50 = 0.013 μM.	29461827
A375	Function assay		Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation by AlphaScreen assay, IC50 = 0.044 μM.	29461827
A375	Function assay		Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK, IC50 = 0.046 μM.	22808911
A375	Antiproliferative assay		Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras, IC50 = 0.5 μM.	22808911
A375	Cytotoxicity assay	72 hrs	Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.5 μM.	29461827
HCT116	Antiproliferative assay		Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant, IC50 = 27 μM.	22808911
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	413.83	Formula	C₁₇H₁₄ClF₂N₃O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	918505-84-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)Cl)F

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (200.56 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.
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.
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:

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% DMSO + % + % Tween 80 + % ddH₂O

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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	C-Raf-1 (Y340D/Y341D) (Cell-free assay) 6.7 nM B-Raf (V600E) (Cell-free assay) 13 nM BRK (Cell-free assay) 130 nM B-Raf (Cell-free assay) 160 nM
In vitro	PLX-4720 displays >10 times selectivity against wild type B-Raf, and >100 times selectivity over other kinases such as Frk, Src, Fak, FGFR, and Aurora A with IC50 of 1.3-3.4 μM. This compound significantly inhibits the ERK phosphorylation in cell lines bearing B-Raf^V600E with IC50 of 14-46 nM, but not the cells with wild-type B-Raf. It significantly inhibits the growth of tumour cell lines bearing the B-Raf^V600E oncogene, such as COLO205, A375, WM2664, and COLO829 with GI50 of 0.31 μM, 0.50 μM, 1.5 μM, and 1.7 μM, respectively. In addition, this chemical treatment at 1 μM induces cell cycle arrest and apoptosis exclusively in the B-Raf^V600E-positive 1205Lu cells, but not in the B-Raf wild-type C8161 cells. This compound treatment (10 μM) significantly induces >14-fold expression of BIM in the PTEN⁺ cells, compared with the PTEN- cell lines (4-fold), giving an explanation of the resistance of PTEN^- cells to this chemical-induced apoptosis.
Kinase Assay	In vitro Raf kinase activities
Kinase Assay	The in vitro kinase activities of wild type Raf and mutants are determined by measuring phosphorylation of biotinylated-MEK protein using Perkin-Elmer's AlphaScreen Technology. For each enzyme (0.1 ng), 20-μL reactions are carried out in 20 mM Hepes (pH 7.0), 10 mM MgCl₂, 1 mM DTT, 0.01% Tween-20, 100 nM biotin-MEK protein, various ATP concentrations, and increasing concentrations of PLX-4720 at room temperature. Reactions are stopped at 2, 5, 8, 10, 20, and 30 minutes with 5 μL of a solution containing 20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, and 0.3% BSA. The stop solution also includes phospho-MEK Antibody, Streptavidin-coated Donor beads and Protein A Acceptor beads from the AlphaScreen Protein A Detection Kit. The antibody and beads are preincubated in stop solution in the dark at room temperature for 30 minutes. The final dilution of antibody is 1/2,000, and the final concentration of each bead is 10 μg/mL. The assay plates are incubated at room temperature for one hour then are read on a PerkinElmer AlphaQuest reader.
In vivo	Oral administration of PLX-4720 at 20 mg/kg/day induces significant tumour growth delays and regressions in B-Raf^V600E-dependent COLO205 tumour xenografts, without obvious adverse effects in mice even at a dose of 1 g/kg. This compound at 100 mg/kg twice daily almost completely eliminates the 1205Lu xenografts bearing B-Raf^V600E, while having no activity against C8161 xenografts bearing wild-type B-Raf. The anti-tumour effects of this compound correlate with the blockade of MAPK pathway in those cells harbouring the V600E mutation. This chemical treatment at 30 mg/kg/day significantly inhibits the tumour growth of 8505c xenografts by >90%, and dramatically decreases distant lung metastases.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18287029/ [2] https://pubmed.ncbi.nlm.nih.gov/21317224/ [3] https://pubmed.ncbi.nlm.nih.gov/20498063/

Applications

Methods	Biomarkers	PMID
Western blot	p-MEK / MEK / p-ERK / ERK / p-FAK(S910) p-EGFR 1173 / EGFR / p-Akt / Akt p27 / Cyclin D1 / pRb pAkt(Ser473) / pAkt(Thr308)	23076151
Immunofluorescence	LAMP1 ZKSCAN3 / TFEB	30979895
Growth inhibition assay	Cell viability	27848137
ELISA	mIFN-γ	23204132

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

Question 1:
What would you recommend to make working solution for intraperitoneal injection into mice?

Answer:
Due to its very limited solubility in aqueous solution, this compound can be administered as a not fully dissolved suspension via oral gavage. For this reason, we recommend oral gavage for its administration.

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