Name: SKLB1002
Brand: Selleck Chemicals
SKU: S7258
Rating: 5 (5 reviews)

Jump to

Quality Control

Batch: Purity: 99.58%

99.58

Related Targets	EGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Other VEGFR Inhibitors	SAR131675 SU 5402 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Anlotinib (AL3818) Dihydrochloride Linifanib (ABT-869) Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 ZM 323881 HCl

Chemical Information, Storage & Stability

Molecular Weight	320.39	Formula	C₁₃H₁₂N₄O₂S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1225451-84-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=NN=C(S1)SC2=NC=NC3=CC(=C(C=C32)OC)OC

Solubility

In vitro
Batch:

DMSO : 4 mg/mL (12.48 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.
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.	0.200mg/ml (0.62mM)	Taking the 1 mL working solution as an example, add 50 μL of 4 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.	0.100mg/ml (0.31mM)	Taking the 1 mL working solution as an example, add 50 μL of 2 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	VEGFR2 32 nM
In vitro	SKLB1002 shows strikingly lower cytotoxicity on normal human cells L-02. This compound significantly inhibits HUVEC proliferation, migration, invasion, and tube formation, by inhibiting VEGF-induced phosphorylation of VEGFR2 kinase and the downstream Protein Tyrosine Kinase including ERK, FAK, and Src.
Kinase Assay	Kinase inhibition assays
Kinase Assay	Kinase inhibition is measured by the use of radiometric assays conducted by Kinase Profiler service. Briefly, in the presence or absence of SKLB1002, VGFR2 (5–10 mU) is incubated in 25-μL reaction solution containing 8 mmol/L 3-(N-morpholino)propanesulfonic acid (MOPS), pH 7.0, 0.2 mmol/L EDTA, 0.33 mg/mL myelin basic protein, 10 mmol/L Mg acetate, and γ-[³³P]ATP. After incubation for 40 minutes at room temperature, the reaction is stopped and 10 μL of the reaction solution is then spotted onto a P30 filtermat and washed 3 times for 5 minutes in 75 mmol/L phosphoric acid and once in methanol prior to scintillation counting.
In vivo	In the zebrafish embryos, SKLB1002 remarkably blocks the formation of embryonic and tumour-induced angiogenesis with no or least impact on normal cell proliferation. In athymic mice bearing SW620 or HepG2 xenografts, this compound (100 mg/kg daily, i.p.) causes significant inhibition of tumour growth, inhibits tumour angiogenesis and induces tumour apoptosis. In 4T1 and CT26 tumour model, this chemical and local hyperthermia produce a synergistic antiangiogenesis, anticancer and promotion of apoptosis efficacy.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21622720/ [2] https://pubmed.ncbi.nlm.nih.gov/23263406/

Tech Support

Handling Instructions

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

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

SKLB1002 VEGFR inhibitor

Chemical Structure

Molecular Weight: 320.39