Cobimetinib
Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
Product Specifications
CAS Number
[934660-93-2]
Product Name Alternative
GDC-0973; XL518
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis; MEK
Type
Reference compound
Related Pathways
Apoptosis; MAPK/ERK Pathway
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Cobimetinib.html
Purity
99.81
Solubility
DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
OC1([C@H]2NCCCC2)CN(C1)C(C3=C(C(F)=C(C=C3)F)NC4=C(C=C(C=C4)I)F)=O
Molecular Formula
C21H21F3IN3O2
Molecular Weight
531.31
Precautions
H302, H315, H319, H335
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]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.|[3]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.|[4]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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
MEK1
Citation 01
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