ARRY-424704, ARRY-704 Chemical Properties

Density 

1.732

storage temp. 

Store at -20°C

solubility 

≥23.05 mg/mL in DMSO; insoluble in H2O; ≥46.1 mg/mL in EtOH

form 

solid

pka

14.31±0.10(Predicted)

color 

Off-white to pink

Safety Information

HS Code 

2933998090

ARRY-424704, ARRY-704 Usage And Synthesis

Description

AZD 8330 is a selective allosteric inhibitor of MEK1/2 (IC₅₀ = 7 nM). It blocks phosphorylation of ERK1/2 and inhibits proliferation of certain cancer cells. AZD 8330 is orally bioavailable, inhibits ERK phosphorylation in vivo, and reduces tumor growth in a Calu-6 nude rat xenograft model.

Uses

AZD8330 is an orally active and selective MEK inhibitor.

Definition

ChEBI: 2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-3-pyridinecarboxamide is a pyridinecarboxamide. It is functionally related to a nicotinamide.

in vivo

target

ERK phosphorylation

IC 50

MEK1: 7 nM (IC₅₀); MEK2: 7 nM (IC₅₀)

References

1. feng k, wang c, zhou h, yang j, dong l, zhou k, et al. [effect of erk1/2 inhibitor azd8330 on human burkitt's lymphoma cell line raji cells and its mechanism]. zhonghua xue ye xue za zhi 2015,36:148-152.2. cohen rb, aamdal s, nyakas m, cavallin m, green d, learoyd m, et al. a phase i dose-finding, safety and tolerability study of azd8330 in patients with advanced malignancies. eur j cancer 2013,49:1521-1529.

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