Cat No.
CEI-0147
Description
AZD8330 can inhibit MEK1/2 with IC50 of 7nM.
CAS No.
869357-68-6
Targets
MEK1/2
Chemical Name
2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide
M.Wt
461.23
Purity
>99%
Solubility
DSMO 92 mg/mL Water
Storage
2 years at -20 centigrade
In vitro
AZD8330 (ARRY-424704),a potent and selective uncompetitive inhibitor, can inhibit MEK1/2 with IC50 of 7 nM and shows inhibition to ERK phosphorylation in Malme-3M cells with IC50 of 0.4 nM.AZD8330 (ARRY-424704) shows sub-nM inhibition of Ras/Raf/MEK/ERK signaling in tumor cell lines and low to sub-nM potency in functional (proliferation) assays in MEK 1/2 inhibitor sensitive cell lines. AZD8330 (ARRY-424704) also inhibit HT29 cell viability, Calu-6 cell viability, and Colo205 cell viability with IC50 of 3.8 nM, 11 nM and 0.7 nM. In tumor cell line panels AZD8330 demonstrates a similar pattern of activity with respect to BRAF and RAS gene mutation status to other MEK 1/2 inhibitors (AZD6244 and PD-0325901).
In vivo
In two nude rat human tumor xenograft models, AZD8330 (oral doses:0.4 mg/kg) shows significant anti-tumor efficacy.
