3-[(2,4-Dimethylpyrrol-5-yl)methylidene]-indolin-2-one
SU5416
Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor III Yellow orange solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable indolinone compound that acts as a selective, ATP-competitive inhibitor of VEGF-R (KDR/Flk-1) and PDGF-R tyrosine kinases (IC50 = 1.04 µM and 20 µM in NIH 3T3 cells overexpressing Flk-1; Km = 530 nM for ATP). Also potently inhibits the proliferation of HUVECs induced by VEGF, bFGF, or ECGS (IC50 = 50 nM, 5.3 µM and 30.5 µM, respectively). Blocks the autophosphorylation of internal tandem duplication (ITD) and wild type Fms-like tyrosine kinase 3 (FLT3) with an IC50 of 0.1 µM. Does not affect the EGF- or FGF- receptor tyrosine kinases activities even at 100 µM concentration. Reported to induce apoptosis and inhibit VEGF-dependent mitogenesis of human endothelial cells. Purity: ≥97% by HPLC. CAS 204005-46-9. Ref.: Tille, J.C., et al. 2003. Exp. Cell Res. 285, 286. Itokawa, T., et al. 2002. Mol. Cancer Ther. 1, 295. Ma, J., et al. 2002. J. Pharmacol. Exp. Ther. 305, 833. Yee, K.W., et al. 2002. Blood 100, 2941. Mendel, D.B., et al. 2000. Clin. Cancer Res. 6, 4848. Fong, T.A.T., et al. 1999. Cancer Res. 59, 99. Sun, L., et al. 1999. J. Med. Chem. 42, 5120. |
