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Merck
CN

676505

VEGFR2 Kinase Inhibitor VII, SKLB1002

The VEGFR2 Kinase Inhibitor VII, SKLB1002 controls the biological activity of VEGFR2 Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

VEGFR2 Kinase Inhibitor VII, SKLB1002, 6,7-Dimethoxy-4-(5-methyl-1,3,4-thiadiazol-2-ylthio)quinazoline, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor VII, SKLB1002, VEGFR Tyrosine Kinase Inhibitor XXXV

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关于此项目

经验公式(希尔记法):
C13H12N4O2S2
分子量:
320.39
NACRES:
NA.77
UNSPSC Code:
12352200
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assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 2.5 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

General description

A cell-permeable quinazoline that acts as a potent, ATP-binding site-targeting, VEGFR2-selective inhibitor (IC50 = 32 nM), while exhibiting much reduced potency against c-kit, Ret, FMS, PDGFRα, and Aurora A (IC50 = 0.62, 2.5, 2.9, 3.1, and 3.9 µM, respectively) and little or no activity against 11 other kinases (IC50 >10 µM). An effective antiangiogenesis agent (86%, 92%, and 98% inhibition, respectively, of HUVEC migration, invasion, and tube formation at 10 µM; 80% inhibition of zebrafish embryos intersegmental vessel growth at 2.5 µM) that significantly suppresses SW620- and HepG2-derived tumor growth in mice (by 72% and 63%, respectively, in 18 days; 100 mg/kg/day; i.p.) in vivo.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Zhang, S., et al. 2011. Clin. Cancer Res.17, 4439.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Regulatory Review (Z)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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