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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Aurora Kinase-LY3295668
LY3295668

Chemical Structure : LY3295668

CAS No.: 1919888-06-4

LY3295668 (LY-329566, AK-01)

货号: PC-35756Not For Human Use, Lab Use Only.

LY3295668 (LY-3295668, AK-01) is a novel potent, highly selective, orally active Aurora-A kinase inhibitor with Ki of 0.8 nM, H446 AurA auto-P IC50 of 0.6 nM.

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

生物&药学活性

LY3295668 (LY-3295668, AK-01) is a novel potent, highly selective, orally active Aurora-A kinase inhibitor with Ki of 0.8 nM, H446 AurA auto-P IC50 of 0.6 nM.
LY3295668 displays >1000-fold selectivity over Aur-B, 5/386 kinases were potently inhibited by LY3295668 (<10 nM) and none of these kinases overlapped with targets of the other AurAi (MK5108, alisertib), and no inhibition of SYK.
LY3295668 is cytotoxic to RB1 mutant cancer cancaer cells (NCI-H446 cell IC50=0.752 uM), causes durable regression of RB1mut tumor xenografts.

物理化学性质&存储条件

分子量 489.952
分子式 C24H26ClF2N5O2
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

(2R,4R)-1-(3-chloro-2-fluorobenzyl)-4-((3-fluoro-6-((5-methyl-1H-pyrazol-3-yl)amino)pyridin-2-yl)methyl)-2-methylpiperidine-4-carboxylic acid

参考文献

1. Gong X, et al. Cancer Discov. 2018 Oct 29. pii: CD-18-0469.

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