产品描述:
PD 082106 is an inhibitor of FMS-related tyrosine kinase 3 (FLT3; IC50 = 0.015 µM, respectively) and a derivative of indirubin (Item No. 14155).{18155} It is selective for FLT3 over Met, Ron, EGFR, and the insulin receptor (IC50s = >10 µM for all) but does inhibit DRAK2 (IC50 = 0.62 µM), as well as VEGFR2 and Aurora A (IC50s = 1.53 and 1.27 µM, respectively).{18155,46931} PD 082106 inhibits proliferation of A549 lung, SNU-638 stomach, HT-1080 fibrosarcoma, HL-60 leukemia, and MCF-7 breast cancer cells with IC50 values of 13, 2.1, 3.4, 89, and 9 µM, respectively, but does not inhibit proliferation of Col 2 colon cancer cells.{46932} It also inhibits proliferation of (IC50 = 5.1 µM), and induces apoptosis in, K-Ras-transformed RK3D rat kidney epithelial (RK3E-ras) cells and reduces tumor growth in RK3E-ras flank and oral tumor models.{46933} PD 082106 is active against the parasite T. gondii (ID50 = 0.52 µM) with a toxic dose value (TD50) of 61 µM.{46934}