AMG 925 (FLX925; AMG925)

Description: AMG 925 (also called FLX-925; AMG-925) is a novel, potent, selective and orally bioavailable FLT3/CDK4 dual inhibitor with potential antitumor activity. It inhibits FLT3/CDK4 with an IC50 of 1 nM and 3 nM, respectively. AMG 925 exhibits excellent anti-proliferative activity in vitro and inhibits cell growth with IC50 values of 19nM and 18nM, respectively, through inhibiting P-FLT3 and P-STAT5 and inducing apoptosis. It also has high in vivo antitumor efficacy in AML tumor–bearing mice, administration of AMG 925 shows inhibition of P-STAT5 and P-RB as well as cell growth both in subcutaneous MOLM13 xenograft tumor model and systemic MOLM13-Luc xenograft tumor model.

References: Mol Cancer Ther. 2014 Apr; 13(4):880-9.

Related CAS: 1401034-19-2 (HCl Salt)

Chemical Name: 2-hydroxy-1-(2-((9-((1r, 4r)-4-methylcyclohexyl)-9H-pyrido[4', 3':4, 5]pyrrolo[2, 3-d]pyrimidin-2-yl)amino)-7, 8-dihydro-1, 6-naphthyridin-6(5H)-yl)ethanone

InChi Key: BBUVDDPUURMFOX-SAABIXHNSA-N

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-

SMILES Code: C[CH]1CC[CH](N2C3=CN=CC=C3C4=CN=C(NC5=NC6=C(CN(C(CO)=O)CC6)C=C5)N=C42)CC1