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.

• Synonyme(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
• Formule empirique (notation de Hill): C₁₃H₁₂N₄O₂S₂
• Poids moléculaire : 320.39
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 2.5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C

Description

Description générale

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.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Regulatory Review (Z)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable