Cobimetinib-d4 (hydrochloride)

Cobimetinib-d4 hydrochloride is deuterated labeled Cobimetinib (HY-13064) . Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.

Product Specifications

Product Name Alternative

GDC-0973-d4 (hydrochloride) ; XL518-d4 (hydrochloride)

UNSPSC

12352005

Target

Apoptosis; Isotope-Labeled Compounds; MEK

Type

Isotope-Labeled Compounds

Related Pathways

Apoptosis; MAPK/ERK Pathway; Others

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Purity

99.26

Solubility

10 mM in DMSO

Smiles

OC1(C([2H])(N(C(C2=C(NC3=C(F)C=C(I)C=C3)C(F)=C(F)C=C2)=O)C1([2H])[2H])[2H])[C@H]4NCCCC4.Cl

Molecular Formula

C21H18D4ClF3IN3O2

Molecular Weight

571.80

References & Citations

[1]Hoeflich KP, et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res. 2012 Jan 1;72 (1) :210-9.|[2]Corazao-Rozas P, et al. Mitochondrial oxidative phosphorylation controls cancer cell's life and death decisions upon exposure to MAPK inhibitors. Oncotarget. 2016 Feb 29. doi: 10.18632/oncotarget.7790.|[3]Choo EF, et al. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71 (1) :133-43.|[4]Wong H, et al. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor. Clin Cancer Res. 2012 Jun 1;18 (11) :3090-9.|[5]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.