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LY-3214996 (LY3214996)
LY-3214996 (Temuterkib) is an orally bioavailable, potent and highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to LY3214996. In tumor xenograft models, LY3214996 inhibits PD biomarker phospho-p90RSK1 in tumors and the PD effects are correlated with compound exposures and anti-tumor activities (ref. 1). It is currently in clinical evaluations.
Catalog NO: CT-LY321
Synonym: Temuterkib
CAS NO: 1951483-29-6
Mol. Formula: C22H27N7O2S
MW: 453.6 (or refer to Certificate of Analysis, batch specific)
** 99.9% Purity. in vivo Quality material. Clean and impeccable. Hemihydrate, Validated by a spot-on Quantitative Elemental Analysis. Bulk Stock! Prompt.