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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.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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