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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FLT3-AMG 925
AMG 925

Chemical Structure : AMG 925

CAS No.: 1401033-86-0

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AMG 925 (AMG-925, AMG925)

货号: PC-26046Not For Human Use, Lab Use Only.

AMG 925 (AMG925, AMG-925) is a potent and orally bioavailable dual inhibitor of CDK4 and FLT3 with IC50 of 3 nM and 1 nM for CDK4/Cyclin D1 and FLT3 respectively.

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10 mg ￥880 In stock
25 mg ￥1380 In stock
50 mg ￥2280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AMG 925 (AMG925, AMG-925) is a potent and orally bioavailable dual inhibitor of CDK4 and FLT3 with IC50 of 3 nM and 1 nM for CDK4/Cyclin D1 and FLT3 respectively.
AMG 925 (AMG925, AMG-925) much weakly inhibits CDK1/Cyclin B (IC50=2.2 uM).
AMG 925 (AMG925, AMG-925) shows high affinity for a panel of activated variants of FLT3 with Kd of 1-4 nM (FLT3ITD, FLT3D835Y, FLT3D835H, FLT3K663Q, FLT3 N841I).
AMG 925 (AMG925, AMG-925) inhibited pSTAT5 in MOLM13 and pRb in Colo205 with IC50s of 0.005 and 0.023 μM, respectively.
AMG 925 induced apoptosis in FLT3ITD AML cell lines and the FLT3ITD,D835Y mutant AML cell line.
AMG 925 showed significant growth inhibition of MOLM13 xenografts in nude mice, and the activity correlates with inhibition of STAT5 and Rb phosphorylation.

物理化学性质&存储条件

分子量 471.57
分子式 C26H29N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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)ethan-1-one

参考文献

1. Li Z, et al. J Med Chem. 2014 Apr 24;57(8):3430-49.

2. Keegan K, et al. Mol Cancer Ther. 2014 Apr;13(4):880-9.

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