GDC-0623
GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM) .
Product Specifications
CAS Number
1168091-68-6
Product Name Alternative
RG 7421; MEK inhibitor 1
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/GDC-0623.html
Concentration
10mM
Purity
98.74
Solubility
DMSO : 50 mg/mL (ultrasonic)
Smiles
FC(C=C(I)C=C1)=C1NC2=C(C(NOCCO)=O)C=CC3=CN=CN23
Molecular Formula
C16H14FIN4O3
Molecular Weight
456.21
Precautions
H302, H315, H319, H335
References & Citations
[1]Hatzivassiliou G, et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature. 2013 Sep 12;501 (7466) :232-6.|[2]Takahashi RH, et al. Elucidating the Mechanisms of Formation for Two Unusual Cytochrome P450-Mediated Fused Ring Metabolites of GDC-0623, a MAPK/ERK Kinase Inhibitor. Drug Metab Dispos. 2015 Dec;43 (12) :1929-1933.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
MEK1
Available Sizes
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