Chemical Structure : Abemaciclib
CAS No.: 1231929-97-7
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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25 mg | ¥880 | In stock | |
50 mg | ¥1180 | In stock | |
100 mg | ¥1580 | In stock | |
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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.
分子量 | 506.61 | |
分子式 | C27H32F2N8 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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 |
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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