BMS 690514

BMS 690514 is a pan-inhibitor of HER and VEGFR family kinases (IC50s = 5, 19, 60, 50, 50, and 25 nM for EGFR, HER2, HER4, VEGFR1, VEGFR2, and VEGFR3, respectively). It is selective for these kinases over 11 additional kinases but also inhibits FMS-related tyrosine kinase 3 (FLT3), calcium/calmodulin-dependent protein kinase II (CAMKII), LCK, and PKA (IC50s = 110, 170, 220, and 280 nM, respectively). BMS 690514 selectively inhibits the proliferation of cancer cells containing EGFR gene amplifications or mutations and HER2 gene amplifications over those expressing wild-type EGFR or not expressing EGFR and HER2. It inhibits tumor growth and angiogenesis in an L2987 lung cancer mouse xenograft model when administered at a dose of 90 mg/kg. Formal Name: (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]-3-piperidinol. CAS Number: 859853-30-8. Molecular Formula: C19H24N6O2. Formula Weight: 368.4. Purity: >98%. Formulation (Request formulation change): A solid. Solubility: Acetonitrile:Water (1:1): Slightly soluble: 0.1-1 mg/ml. SMILES: COC1=CC=CC(NC2=NC=NN(C=C3)C2=C3CN4CC[C@H]([C@@H](C4)O)N)=C1. InChi Code: InChI=1S/C19H24N6O2/c1-27-15-4-2-3-14(9-15)23-19-18-13(5-8-25(18)22-12-21-19)10-24-7-6-16(20)17(26)11-24/h2-5,8-9,12,16-17,26H,6-7,10-11,20H2,1H3,(H,21,22,23)/t16-,17-/m1/s1. InChi Key: CSGQVNMSRKWUSH-IAGOWNOFSA-N. Storage: -20°C. Stability: > 4 years.