AMG-925 is a potent and orally bioavailable dual inhibitor of CDK4 and FLT3, including many FLT3 mutants reported to date. It inhibits the proliferation of a panel of human tumor cell lines including Colo205 (Rb(+)) and U937 (FLT3(WT)) and induced cell death in MOLM13 (FLT3(ITD)) and even in MOLM13 (FLT3(ITD, D835Y)), which exhibits resistance to a number of FLT3 inhibitors currently under clinical development. At well-tolerated doses, AMG 925 leads to significant growth inhibition of MOLM13 xenografts in nude mice, and the activity correlates with inhibition of STAT5 and Rb phosphorylation.
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| 名称 | AMG-925 |
|---|---|
| Iupac 化学名称 | 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 |
| 同义词 | AMG-925 ; AMG925 ; AMG 925 |
| 英文同义词 | AMG-925 ; AMG925 ; AMG 925 |
| 分子式 | C26H29N7O2 |
| 分子量 | 471.55 |
| Smile | C[C@H]1CC[C@H](N2C3=CN=CC=C3C4=CN=C(NC5=NC6=C(CN(C(CO)=O)CC6)C=C5)N=C42)CC1 |
| InChiKey | BBUVDDPUURMFOX-SAABIXHNSA-N |
| InChi | 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- |
| Cas号 | 1401033-86-0 |
| 相关CAS号 | 1401034-19-2 ( HCl) ; 1401033-86-0 (free) |
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 类白色至白色固体 |
|---|---|
| 纯度 | 98% |
| 存储 | 3 years -20ºCpowder |
| 可溶性 | Soluble in DMSO |
| 处理方式 | |
| 运输条件 | Shipped under ambient temperature |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1.J Med Chem. 2014 Apr 24;57(8):3430-49. doi: 10.1021/jm500118j. Epub 2014 Apr 2.