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Background Information:
LY-3214996 (LY3214996) 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.
Reference:
1. S. V. Bhagwat, et al. Abstract 4973: Discovery of LY3214996, a selective and novel ERK1/2 inhibitor with potent antitumor activities in cancer models with MAPK pathway alterations. Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 4973. doi:10.1158/1538-7445.AM2017-4973.
APIM050041: LY-3214996 (LY3214996)
CAS No.: 1951483-29-6.
Molecular Formula: C22H27N7O2S.
Molecular Weight: 453.6 (or refer to Certificate of Analysis, batch specific).
Purity: >99.7% (HPLC at 214 and 254 nm).
QC: HPLC, NMR and Quantitative Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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