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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-Abemaciclib
Abemaciclib

Chemical Structure : Abemaciclib

CAS No.: 1231929-97-7

Abemaciclib (LY2835219, LY 2835219)

货号: PC-20589Not For Human Use, Lab Use Only.

Abemaciclib (LY2835219) is a potent, selective and ATP-competitive CDK4/6 inhibitor with Ki values of 0.6 and 2.4 nM for CDK4/cyclin D1 and CDK6/cyclin D1, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Abemaciclib (LY2835219) is a potent, selective and ATP-competitive CDK4/6 inhibitor with Ki values of 0.6 and 2.4 nM for CDK4/cyclin D1 and CDK6/cyclin D1, respectively.
Abemaciclib (LY2835219) inhibits CDK4/cyclin D1 and CDK6/cyclin D1 with IC50 of 2 and 10 nM, respectively, with high selectivity against CDK1/cyclin B1, CDK2/cyclin E, and CDK7/Mat1/cyclin H.
Abemaciclib (LY2835219) is a potent inhibitor of Rb phosphorylation (IC50=120 nM) in colo-205 cells, induces a complete cell cycle arrest and suppresses expression of several Rb-E2F-regulated proteins.
Abemaciclib (LY2835219) inhibits tumor growth in human tumor xenografts representing different histologies in tumor-bearing mice.
Abemaciclib (LY2835219) in combination with gemcitabine enhanced in vivo antitumor activity without a G1 cell cycle arrest in calu-6 xenografts.

物理化学性质&存储条件

分子量 506.61
分子式 C27H32F2N8
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

N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine

参考文献

1. Tate SC, et al. Clin Cancer Res. 2014 Jul 15;20(14):3763-74.

2. Gelbert LM, et al. Invest New Drugs. 2014 Oct;32(5):825-37.

3. Yadav V, et al. Mol Cancer Ther. 2014 Oct;13(10):2253-63.

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