RGNCY-0027 ((S)-14K)

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(S)-14k is pyridone ERK1/2 inhibitor optimized to be a potent, selective and orally bioavailable agent that inhibited tumor growth in mouse xenograft models. On the basis of its in vivo efficacy and preliminary safety profiles in several sepcies, (S)-14k was selected for further preclinical evaluation.  ErK2 enzyme Ki = 0.3+0.02 nM, CDK2 enzyme Ki = 21+8 nM, Phospho-p90RSK = 17+4 nM.

Systematic Name: (S)-1-(1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one

SMILES: O=C1N([C@H](CO)C2=CC(F)=C(Cl)C=C2)C=CC(C3=NC(NC4CCOCC4)=NC=C3)=C1

Chemical Formula: C22H22ClFN4O3

Molecular Weight: 444.89

PMID: 25603482

Reference: Ren, Li, et al. "Discovery of Highly Potent, Selective and Efficacious Small Molecule Inhibitors of ERK1/2." Journal of Medicinal Chemistry (2015).

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