GDC-0973 (COBIMETINIB)

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.