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.