AZD8330

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Cat No.

CEI-0147

Description

AZD8330 can inhibit MEK1/2 with IC50 of 7nM.

CAS_No

869357-68-6

Molecular Weight

461.23

Purity

>99%

Storage

2 years at -20 centigrade

Targets

MEK1/2

Molecular Formula

C16H17FIN3O4

Chemical Name

2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide

Solubility

DSMO 92 mg/mL Water

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.

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Our Products Cannot Be Used As Medicines Directly For Personal Use.

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