3-(1H-Pyrrol-2-ylmethylene)-1,3-dihydroindol-2-one Orange solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A potent and selective inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinase Flk-1 (fetal liver kinase-1; IC50 = 390 nM). Also, to a lesser extent, it inhibits platelet derived growth factor receptor (PDGFR) kinase (IC50 = 12 µM). However, it does not affect EGFR, HER2, and IGF-1R even at high concentrations (>100 µM). Also inhibits cyclin D1/Cdk4 enzyme (IC50 = 4.9 µM) preferentially over cyclin E/Cdk2 (IC50 = 10 µM) and cyclin B/Cdk1 (IC50 = 10.2 µM). Purity: ≥95% by HPLC. Ref.: Kent, L.L., et al. 1999. Biochem. Biophys. Res. Commun. 260, 768. Sun, L., et al. 1998. J. Med. Chem. 41, 2588. |
