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Astex ERK inhibitor X

Chemical Structure : Astex ERK inhibitor X

CAS No.: 2095719-90-5

Astex ERK inhibitor X

Catalog No.: PC-63537Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 550.056
Formula C29H32ClN5O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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