AMG 925 HCl
A dual inhibitor of FLT3 and Cdk4
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包装价格促销价数量
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5mg￥925.00740.00- +
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10mg￥1300.001040.00- +
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50mg￥3775.003020.00- +
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100mg￥5937.004750.00- +
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200mg￥0.000.00- +
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500mg￥0.000.00- +
- 货号: ajce54872
- CAS: 1401034-19-2
- 别名:
- 分子式: C26H30ClN7O2
- 分子量: 508.02
- 纯度: ＞98%
- 溶解度: DMSO: 1 mg/mL (1.97 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
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).1 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.
1.Li, Z., Wang, X., Eksterowicz, J., et al.Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3J. Med. Chem.57(8)3430-3439(2014)
