Cabozantinib, Met and VEGFR2 inhibitor (TBI3231)

Description

Product Details

Formal Name: N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Alternate Names: XL-184; BMS-907351

Molecular Formula: C₂₈H₂₄FN₃O₅

Formula Weight: 501.51

CAS Number: 849217-68-1

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO.

Storage: -20°C

Stability: ≥ 1 year.

Applications

Met and VEGFR2 inhibitor

Functions

Novel inhibitor of c-met and VEGFR2 kinase activity, IC50=3.5 nm and 35 pM respectively. Inhibits MET-activating kinase domain mutations Y1248H, D1246N or K1262R, IC50=3.8, 11.8 and 14.6 nM respectively. In cellular assays it inhibits the following kinases: MET, VEGF2, KIT, FLT3 and AXL, IC50=7.8, 1.9, 5.0, 7.5 and 42 μM respectively. Eliminated approximately 80% of vasculature in spontaneous pancreatic islet tumors over 7 days in a mouse model. Clinically useful anticancer agent.

Application Procedures

First dissolved in DMSO, then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 1 month.