AMG 925

AMG 925 is a dual inhibitor of FMS-related tyrosine kinase 3 (FLT3) and cyclin-dependent kinase 4 (Cdk4, IC50s = 1 and 3 nM, respectively). It is selective for FLT3 and Cdk4 over Cdk1 (IC50 = 2.22 µM). AMG 925 also binds to FLT3ITD, FLT3D835Y, FLT3D835H, FLT3K663Q, and FLT3N841I (Kds = 1-4 nM). It inhibits proliferation of MOLM-13, COLO 205, and U937 cancer cells (IC50s = 19, 55, and 52 nM, respectively). AMG 925 (50, 75, and 150 mg/kg) reduces intratumor levels of pSTAT5 and pRb and inhibits tumor growth in a MOLM-13 acute myeloid leukemia (AML) mouse xenograft model.Formal Name: 1-[7,8-dihydro-2-[[9-(trans-4-methylcyclohexyl)-9H-pyrido[4',3':4,5]pyrrolo[2,3-d]pyrimidin-2-yl]amino]-1,6-naphthyridin-6(5H)-yl]-2-hydroxy-ethanone. CAS Number: 1401033-86-0. Molecular Formula: C26H29N7O2. Formula Weight: 471.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: Chloroform: 500µg/ml. lambdamax: 227, 268, 342 nm. SMILES: O=C(CO)N(CC1)CC(C1=N2)=CC=C2NC3=NC=C(C4=N3)C5=CC=NC=C5N4[C@@]6([H])CC[C@H](C)CC6. InChi Code: InChI=1S/C26H29N7O2/c1-16-2-5-18(6-3-16)33-22-13-27-10-8-19(22)20-12-28-26(31-25(20)33)30-23-7-4-17-14-32(24(35)15-34)11-9-21(17)29-23/h4,7-8,10,12-13,16,18,34H,2-3,5-6,9,11,14-15H2,1H3,(H,28,29,30,31)/t16-,18-. InChi Key: BBUVDDPUURMFOX-SAABIXHNSA-N.