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Background Information:
Extracellular signal regulated kinase (ERK) is a pivotal enzyme in the pathway downstream of Ras, Raf, and MEK, acting as a central link between multiple signaling pathways. SCH772984 is a potent, specific and ATP competitive inhibitor of ERK1 and ERK2 with IC50s at low nMs. It inhibits phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phospho-RSK) in a dose-dependent manner, and also inhibits phosphorylation of residues in the activation loop of ERK itself. More importantly, it effectively inhibits MAPK signaling and cell proliferation in BRAF or MEK inhibitor-resistant models as well as in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors (ref. 1).
Reference:
1. E. J. Morris, et al, Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitor, Cancer Discovery , 2013 Jul.3(7):742-50.
2. The optical purity (e.e) of SCH772984 being offered by many other vendors is simply too bad to be reported in their Certificate of Analysis (COA).* Our preparation also yields superior solubility for this product (up to 30 mM).
APIM050237: SCH772984
CAS No.: 942183-80-4.
Molecular Formula: C33H33N9O2.
Molecular Weight: 587.7 (or refer to Certificate of Analysis, batch-specific).
Purity: 100% optical purity (Chiral HPLC), >99% purity (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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