(5-Butanoate-1H-2-indolyl)(1H-2-indolyl)-methanone D-65476 [2-(1H-2-Indolylcarbonyl)-1H-5-indolyl]butanoate Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable bis(1H-2-indolyl)-1-methanone compound that acts as a highly selective, ATP-competitive inhibitor of platelet-derived growth factor (PDGF) receptor tyrosine kinase (IC50 = 1.1 µM in Swiss 3T3 cells for PDGFR). Also potently inhibits Flt3 (Fms-like tyrosine kinase 3) activity (IC50 = 6.2 µM for hPDGFb-R-mFlt3 and 50 nM in EOL-1 cells). Sensitizes 32D cells to radiation-induced apoptosis and inhibits proliferation of TEL-Flt3-transfected BA/F3 cells (IC50 < 300 nM). May also serve as a prodrug form of the Platelet Derived Growth Factor Receptor Tyrosine Kinase Inhibitor I (Cat. No. 521230) in cells. Purity: ≥97% by HPLC. CAS 249762-74-1. Ref.: Mahboobi, S., et al. 2002. J. Med. Chem. 45, 1002. Teller, S., et al. 2002. Leukemia 16, 1528. |