SCH772984

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: C₃₃H₃₃N₉O_2.
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.