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GDC-0623

Chemical Structure : GDC-0623

CAS No.: 1168091-68-6

GDC-0623 (RG 7421, G-868 )

Catalog No.: PC-73145Not For Human Use, Lab Use Only.

GDC-0623 (RG 7421) is a potent, selective, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM).

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Biological Activity

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.

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