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LY3295668 (AK-01) Sale

(Synonyms: AK-01) 目录号 : GC33057

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 (AK-01) Chemical Structure

Cas No.:1919888-06-4

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5mg
¥3,510.00
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10mg
¥6,120.00
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50mg
¥18,360.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

Cas No. 1919888-06-4 SDF
别名 AK-01
Canonical SMILES O=C([C@@]1(CC2=NC(NC3=NNC(C)=C3)=CC=C2F)C[C@@H](C)N(CC4=CC=CC(Cl)=C4F)CC1)O
分子式 C24H26ClF2N5O2 分子量 489.95
溶解度 DMSO : 150 mg/mL (306.15 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.041 mL 10.2051 mL 20.4102 mL
5 mM 0.4082 mL 2.041 mL 4.082 mL
10 mM 0.2041 mL 1.0205 mL 2.041 mL
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Research Update

Selective Inhibition of Aurora Kinase A by AK-01/LY3295668 Attenuates MCC Tumor Growth by Inducing MCC Cell Cycle Arrest and Apoptosis

Cancers (Basel) 2021 Jul 23;13(15):3708.PMID:34359608DOI:PMC8345130

Merkel cell carcinoma (MCC) is an often-lethal skin cancer with increasing incidence and limited treatment options. Although immune checkpoint inhibitors (ICI) have become the standard of care in advanced MCC, 50% of all MCC patients are ineligible for ICIs, and amongst those treated, many patients develop resistance. There is no therapeutic alternative for these patients, highlighting the urgent clinical need for alternative therapeutic strategies. Using patient-derived genetic insights and data generated in our lab, we identified aurora kinase as a promising therapeutic target for MCC. In this study, we examined the efficacy of the recently developed and highly selective AURKA inhibitor, AK-01 (LY3295668), in six patient-derived MCC cell lines and two MCC cell-line-derived xenograft mouse models. We found that AK-01 potently suppresses MCC survival through apoptosis and cell cycle arrest, particularly in MCPyV-negative MCC cells without RB expression. Despite the challenge posed by its short in vivo durability upon discontinuation, the swift and substantial tumor suppression with low toxicity makes AK-01 a strong potential candidate for MCC management, particularly in combination with existing regimens.