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Chemical Structure : Astex ERK inhibitor X
CAS No.: 2095719-90-5
Catalog No.: 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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|---|---|---|---|
| 2 mg | $258 | In stock | |
| 5 mg | $488 | In stock | |
| 10 mg | $758 | In stock | |
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| 100 mg | Get quote |
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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.
| M.Wt | 550.056 | |
| Formula | C29H32ClN5O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Heightman TD, et al. J Med Chem. 2018 Jun 14;61(11):4978-4992. (Compound 27).
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