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首页-小分子抑制剂&激动剂-Tyrosine Kinase-TAM Receptor (Tyro3-Axl-Mer)-A-910
A-910

Chemical Structure : A-910

CAS No.: 3036009-40-9

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A-910 (A910)

货号: PC-23041Not For Human Use, Lab Use Only.

A-910 is a highly potent and selective, orally active dual MerTK/Axl inhibitor with IC50 of 0.2/0.9 nM respectively, >200-fold selective over Tyro3.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

A-910 is a highly potent and selective, orally active dual MerTK/Axl inhibitor with IC50 of 0.2/0.9 nM respectively, >200-fold selective over Tyro3.
A-910 exhibits similar biochemical and Ba/F3 cellular potency (IC50=4.2 nM), shows EC50 of 4.0 and 8.0 nM in in vitro efferocytosis and pMerTK assays respectively.
A-910 exhibits favorable oral bioavailability, exceptional kinome selectivity, and significantly improved in vivo target engagement.

物理化学性质&存储条件

分子量 694.85
分子式 C40H47FN6O4
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

6-Amino-N-[(1S,2S)-2-({4-[(5S)-5-{4-[(2S)-2,3-dihydroxypropyl]piperazin-1-yl}-5,6,7,8-tetrahydronaphthalen-2-yl]phenyl}methoxy)cyclopentyl]-2′-fluoro[3,3′-bipyridine]-5-carboxamide

参考文献

1. Yu Y, et al. J Med Chem. 2024 Sep 16. doi: 10.1021/acs.jmedchem.4c01450.

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