GDC-0623

• Description :

  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 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

• CAS Number :

  [1168091-68-6]