PD 082106

PD 082106 is an inhibitor of FMS-related tyrosine kinase 3 (FLT3, IC50 = 0.015 µM, respectively) and a derivative of indirubin (Cay-14155). 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). 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. 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. PD 082106 is active against the parasite T. gondii (ID50 = 0.52 µM) with a toxic dose value (TD50) of 61 µM.Formal Name: 3-[1,3-dihydro-3-(hydroxyimino)-2H-indol-2-ylidene]-5-fluoro-1,3-dihydro-2H-indol-2-one. CAS Number: 861214-33-7. Synonyms: 5'-FIO, 5'-Fluoroindirubinoxime. Molecular Formula: C16H10FN3O2. Formula Weight: 295.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble. lambdamax: 280, 290 nm. SMILES: FC1=CC=C2C(/C(C(N2)=O)=C3\C(C(C=CC=C4)=C4N3)=N\O)=C1. InChi Code: InChI=1S/C16H10FN3O2/c17-8-5-6-12-10(7-8)13(16(21)19-12)15-14(20-22)9-3-1-2-4-11(9)18-15/h1-7,18,22H,(H,19,21)/b15-13-,20-14+. InChi Key: RJIBTAMXAXHIAN-WAVHTBQISA-N.