Home Protein Tyrosine Kinase VEGFR inhibitor SKLB1002 For research use only.

SKLB1002

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

SKLB1002 Chemical Structure

SKLB1002 Chemical Structure

CAS No. 1225451-84-2

Purity & Quality Control

SKLB1002 Related Products

Signaling Pathway

VEGFR Signaling Pathways

VEGFR Signaling Pathway

Biological Activity

Description SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.
Targets
VEGFR2 [1]
32 nM
In vitro
In vitro SKLB1002 shows strikingly lower cytotoxicity on normal human cells L-02. SKLB1002 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.
Cell Research Cell lines HUVECs, L-02, B16-F10, HepG2, and SW620 cells.
Concentrations ~40 μM
Incubation Time 24 hours
Method Cell proliferation is measured using MTT assay. Various cells including HUVECs, L-02, B16-F10, HepG2, and SW620 are treated with indicated concentrations of SKLB1002 for 24 hours. Vandetanib and sunitinib serve as positive controls. Each assay is replicated 3 times.
In Vivo
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, SKLB1002 (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, SKLB1002 and local hyperthermia produce a synergistic antiangiogenesis, anticancer and promotion of apoptosis efficacy. [2]
Animal Research Animal Models Mice bearing SW620 or HepG2 tumors.
Dosages ~100 mg/kg daily
Administration i.p.

Chemical Information & Solubility

Molecular Weight 320.39 Formula

C13H12N4O2S2
CAS No. 1225451-84-2 SDF --
Smiles CC1=NN=C(S1)SC2=NC=NC3=CC(=C(C=C32)OC)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 4 mg/mL ( (12.48 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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