PD 180970

PD 180970 is an inhibitor of Bcr-Abl. It inhibits wild-type and mutant forms of Bcr-Abl, as well as the p210 isoform, a marker of chronic myelogenous leukemia (CML), with IC50 values ranging from 5 to 48 nM. PD 180970 is selective for Bcr-Abl over basic FGFR (bFGFR) and PDGFR (IC50s = 934 and 1,430 nM, respectively) but also inhibits Src, LCK, KIT, and EGFR (IC50s = 0.8, 1 phase and apoptosis in K562 CML cells when used at a concentration of 50 nM. PD 180970 (500 nM) inhibits constitutive STAT3 DNA-binding activity in, and proliferation of, MDA-MB-468 breast cancer cells. It also inhibits proliferation of Ba/F3 cells expressing mutant p210 Bcr-AblY253F that are resistant to imatinib (Cay-13139) with an IC50 value of 48 nM.Formal Name: 6-(2,6-dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one. CAS Number: 287204-45-9. Molecular Formula: C21H15Cl2FN4O. Formula Weight: 429.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 20 mg/ml. SMILES: CC1=C(F)C=CC(NC2=NC=C(C=C(C3=C(Cl)C=CC=C3Cl)C(N4C)=O)C4=N2)=C1. InChi Code: InChI=1S/C21H15Cl2FN4O/c1-11-8-13(6-7-17(11)24)26-21-25-10-12-9-14(20(29)28(2)19(12)27-21)18-15(22)4-3-5-16(18)23/h3-10H,1-2H3,(H,25,26,27). InChi Key: SLCFEJAMCRLYRG-UHFFFAOYSA-N.