Home Protein Tyrosine Kinase VEGFR inhibitor SKLB1002

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SKLB1002 VEGFR inhibitor

Cat.No.S7258

SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.
SKLB1002 VEGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 320.39

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Chemical Information, Storage & Stability

Molecular Weight 320.39 Formula

C13H12N4O2S2

 Storage (From the date of receipt)
CAS No. 1225451-84-2 -- Storage of Stock Solutions

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

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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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
VEGFR2 [1]
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 kinases including ERK, FAK, and Src. [1]
Kinase Assay
Kinase inhibition assays
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 tumor-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 tumor growth, inhibits tumor angiogenesis and induces tumor apoptosis. [1] In 4T1 and CT26 tumor model, this chemical and local hyperthermia produce a synergistic antiangiogenesis, anticancer and promotion of apoptosis efficacy. [2]
References

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