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Astex ERK inhibitor X

Chemical Structure : Astex ERK inhibitor X

CAS No.: 2095719-90-5

Astex ERK inhibitor X (ERK inhibitor 29)

货号: PC-63537Not For Human Use, Lab Use Only.

Astex ERK inhibitor X (ERK inhibitor 29) is a potent, selective ERK1/2 inhibitor that inhibits ERK catalytic activity with IC50 of 3 nM.

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

生物&药学活性

Astex ERK inhibitor X (ERK inhibitor 29) is a potent, selective ERK1/2 inhibitor that inhibits ERK catalytic activity with IC50 of 3 nM.
Astex ERK inhibitor X displays excellent selectivity toward ERK1/2 against a panel of 429 kinases, only inhibits three kinases inhibited at >50% at 100 nM and 16 kinases at 1 μM.
Astex ERK inhibitor X potently inhibits ERK catalytic activity in NCI-H358 and Calu-6 cells (K-Ras mutant NSCLC) with IC50 of 11 and 15 nM, respectively.
Astex ERK inhibitor X inhibits the proliferation of a panel of KRAS-mutant NSCLC cell lines, 55% of the KRAS-mutant NSCLC cell lines with IC50 of 1-500 nM.
Astex ERK inhibitor X demonstrates in vivo anti-tumor activity in a range of KRAS-mutant NSCLC cancer models.

物理化学性质&存储条件

分子量 550.056
分子式 C29H32ClN5O4
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

(R)-2-(6-(5-chloro-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)-1-oxoisoindolin-2-yl)-N-((S)-2-hydroxy-1-(m-tolyl)ethyl)propanamide

参考文献

1. Heightman TD, et al. J Med Chem. 2018 Jun 14;61(11):4978-4992. (Compound 27).

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