676500-M

VEGFR2/Flt3/c-Kit Inhibitor

The VEGFR2/Flt3/c-Kit Inhibitor, also referenced under CAS 796967-10-7, controls the biological activity of VEGFR2/Flt3/c-Kit. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

• Synonym(s): VEGFR2/Flt3/c-Kit Inhibitor, N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-Nʹ-(3-methylphenyl)urea, Vascular Endothelial Growth Factor Receptor-2/Flt3/c-Kit Inhibitor, Flt-3 Inhibitor V, VEGFR Tyrosine Kinase Inhibitor XXV, VEGFR2 Kinase Inhibitor XXII, c-Kit Inhibitor I, Vascular Endothelial Growth Factor Receptor-2/Flt3/c-Kit Inhibitor, N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-Nʹ-(3-methylphenyl)urea, Flt-3 Inhibitor V, VEGFR Tyrosine Kinase Inhibitor XXV, VEGFR2 Kinase Inhibitor XXII, c-Kit Inhibitor I
• Empirical Formula (Hill Notation): C₂₁H₁₉N₅O
• CAS Number: 796967-10-7
• Molecular Weight: 357.41
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: ethanol: 10 mg/mL; DMSO: 100 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell-permeable 3-aminoindazolylurea compound that acts as a potent and ATP-competitive inhibitor of VEGFR2/KDR (IC₅₀ = 3 nM) as well as Flt3 and cKit (IC₅₀ = 4 to 20 nM). Shown to block VEGF-induced VEGFR2 phosphorylation in 3T3-murine fibroblasts in vitro (IC₅₀ = 13 nM) and exhibit oral availability (AUC = 6.5 µM•h with an oral dose of 10 mg/kg in CD-1 mice) and in vivo efficacy in a murine estradiol-induced uterine edema model (ED₅₀ = 4 mg/kg p.o. in balb/c mice).

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

Dai, Y., et al. 2007. J. Med. Chem.50, 1584.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable