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.

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₁₃H₁₂N₄O₂S₂
• Molecular Weight: 320.39
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• 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

Description

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 or little activity against 16 other kinases. An effective antiangiogenesis agent (98% inhibition of HUVEC 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.

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

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable