Astex ERK inhibitor X

Research use only, not for human use.

Astex ERK inhibitor X is a novel potent ERK1/2 inhibitor that inhibits ERK catalytic activity with IC50 of 3 nM in TRK kinase assays.

Astex ERK inhibitor X is a novel potent ERK1/2 inhibitor that inhibits ERK catalytic activity with IC50 of 3 nM in TRK kinase assays; potently inhibits ERK catalytic activity in NCI-H358 and Calu-6 cells (K-Ras mutant NSCLC) with IC50 of 11 and 15 nM, respectively; 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; demonstrates in vivo anti-tumor activity in a range of KRAS-mutant NSCLC cancer models.

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MAPK/ERK Signaling

ERK

ERK

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2095719-90-5

550.06

C29H32ClN5O4

>98% (HPLC)

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ClC1=CN=C(NC2CCOCC2)N=C1C3=CC=C(CN([C@H](C)C(N[C@H](CO)C4=CC=CC(C)=C4)=O)C5=O)C5=C3

(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

(-20℃)

With Ice Pack

≥ 2 years