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Background Information:
GDC-0973 (Cobimetinib, XL518) is an orally bioavailable, potent and selective small-molecule inhibitor of mitogen-activated protein kinase 1 (MAP2K1 or MEK1). It blocks the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation, and decreased tumor cell proliferation. It is currently being used, in combination with Vemurafenib (PLX4032, our Prod No CT-P4032), in the treatment of unresectable or metastatic melanoma with a BRAF V600E or V600K mutation.
Reference:
1. K. D. Rice, et al, Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973), ACS Med. Chem. Lett., 2012, 3 (5), pp 416–421.
APIM050151: GDC-0973 (COBIMETINIB)
CAS No.: 934660-93-2.
Molecular Formula: C21H21F3IN3O2.
Molecular Weight: 531.3.
Purity: >99% chem and optical purity (by achiral and chiral HPLCs).
QC: Achiral HPLC, 1H-NMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Refer to COA.
Storage: Refer to COA.
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