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- Aurora Kinase
- LY3295668 (AK-01)
LY3295668 (AK-01)
LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.
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包装价格促销价数量
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5mg￥4200.003360.00- +
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10mg￥7337.005870.00- +
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50mg￥21800.0017440.00- +
- 货号: ajcx12876
- CAS: 1919888-06-4
- 别名: AK-01
- 分子式: C24H26ClF2N5O2
- 分子量: 489.95
- 纯度: ＞98%
- 溶解度: DMSO : 150 mg/mL (306.15 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.
LY3295668, an AURKA inhibitor with over 1,000-fold selectivity versus AURKB, is distinguished by minimal toxicity to bone marrow cells at concentrations active against RB1mut cancer cells.[1]
LY3295668 leads to durable regression of RB1mut tumor xenografts at exposures that are well tolerated in rodents. Genetic suppression screens identifi ed enforcers of the spindle-assembly checkpoint (SAC) as essential for LY3295668 cytotoxicity in RB1-defi cient cancers and suggest a model in which a primed SAC creates a unique dependency on AURKA for mitotic exit and survival.[1]
[1] Xueqian Gong, et al. Cancer Discov. 2019 Feb;9(2):248-263.
