869357-68-6

Basic information

• Product Name: ARRY-424704, ARRY-704
• Synonyms: ARRY-424704, ARRY-704;AZD8330;2-(2-Fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide;ARRY424704;ARRY-424704;ARRY704;ARRY-704;AZD8330/ARRY-424704/arry-704/AZD8330/AZD-8330
• CAS NO: 869357-68-6
• Molecular Formula: C₁₆H₁₇FIN₃O₄
• Molecular Weight: 461.23
• EINECS: -0
• Product Categories: Inhibitors;MAPK
• Mol File: 869357-68-6.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• Density: 1.732
• Solubility: ≥23.05 mg/mL in DMSO; insoluble in H2O; ≥46.1 mg/mL in EtOH
• CAS DataBase Reference: ARRY-424704, ARRY-704(CAS DataBase Reference)
• NIST Chemistry Reference: ARRY-424704, ARRY-704(869357-68-6)
• EPA Substance Registry System: ARRY-424704, ARRY-704(869357-68-6)

Safety Data

• Hazardous Substances Data: 869357-68-6(Hazardous Substances Data)

Usage

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.

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.

Upstream product

• 934639-06-2 2-(2-fluoro-4-iodophenylamino)-1,5-dimethyl-6-oxo-N-(2-(vinyloxy)ethoxy)-1,6-dihydropyridine-3-carboxamide 
• 38025-90-0 2-chloro-6-oxo-1,6-dihydropyridine-3-carboxylic acid 
• 853109-24-7 methyl 2-chloro-1-methyl-6-oxo-1,6-dihydropyridine-3-carboxylate 
• 869357-64-2 methyl 2-chloro-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxylate 
• 869357-63-1 methyl 5-bromo-2-chloro-1-methyl-6-oxo-1,6-dihydropyridine-3-carboxylate 
• 869357-67-5 2-(2-fluoro-4-iodo-anilino)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid methyl ester 
• 38496-18-3 2,6-dichloropyridine-3-carboxylic acid 

Relevant articles and documents

COMBINATION THERAPY COMPRISING AZD2171 AND AZD6244 OR MEK-INHIBITOR II

The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of AZD2171 in combination with AZD6244 or MEK Inhibitor II; to a pharmaceutical composition comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II; to a combination product comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II; to the use of AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.

COMBINATION OF AN MEK INHIBITOR AND THE SRC KINASE INHIBITOR AZD0530 FOR USE IN THE TREATMENT OF CANCER

The invention relates to a combination for use in the treatment of cancer comprising a MEK inhibitor and the Src kinase inhibitor AZD0530.

Heterocyclic inhibitors of MEK and methods of use thereof

Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.