Cobimetinib-d4 (hydrochloride)

Cobimetinib-d4 (hydrochloride)

• UNSPSC Description: 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.
• Target Antigen: Apoptosis; Isotope-Labeled Compounds; MEK
• Type: Isotope-Labeled Compounds
• Related Pathways: Apoptosis;MAPK/ERK Pathway;Others
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• 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 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.
• Shipping Conditions: Room temperature
• Clinical Information: No Development Reported