GDC-0623 (RG 7421) is a potent, selective, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM). GDC-0623 displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM), prevents MEK phosphorylation by CRAF in vitro, and able to block MEK phosphorylation by BRAF(V600E). GDC-0623 (RG 7421) (40 mg/kg, p.o.) shows percent tumour growth inhibition (%TGI) in MiaPaCa-2 xenograft model.
Physicochemical Properties
M.Wt
456.21
Formula
C16H14FIN4O3
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Month
Shipping
Solubility
Chemical Name/SMILES
References
1. Hatzivassiliou G, et al. Nature. 2013 Sep 12;501(7466):232-6.
2. Robarge KD, et al. Bioorg Med Chem Lett. 2014 Oct 1;24(19):4714-4723.
3. Zaanan A, et al. J Biol Chem. 2015 Sep 25;290(39):23838-49.
