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

ARRY-424704, also known as ARRY-704, is a selective allosteric inhibitor of MEK1/2 with an IC50 of 7 nM. It effectively blocks the phosphorylation of ERK1/2, a key component in the MAPK/ERK signaling pathway, and inhibits the proliferation of certain cancer cells. ARRY-424704 is orally bioavailable and has demonstrated the ability to inhibit ERK phosphorylation in vivo, as well as reduce tumor growth in a Calu-6 nude rat xenograft model.

Uses

Used in Oncology:
ARRY-424704, ARRY-704 is used as a targeted therapy for cancer treatment, specifically for inhibiting the MEK1/2 enzyme and the subsequent phosphorylation of ERK1/2. This inhibition can lead to the suppression of tumor growth and proliferation in certain cancer types.
Used in Drug Development:
ARRY-424704, ARRY-704 is used as a research tool in the development of new cancer therapies. Its selectivity and potency as a MEK1/2 inhibitor make it a valuable compound for studying the role of the MAPK/ERK signaling pathway in cancer and for evaluating the potential of MEK inhibitors in combination with other targeted therapies or immunotherapies.
Used in Preclinical Models:
ARRY-424704, ARRY-704 is used in preclinical cancer models to assess its efficacy and safety as a potential cancer treatment. It can be employed in various in vitro and in vivo assays to study its impact on tumor growth, metastasis, and resistance to therapy, as well as its potential synergistic effects when combined with other drugs.
Used in Personalized Medicine:
ARRY-424704, ARRY-704 can be used in the context of personalized medicine to identify patients who are most likely to benefit from MEK inhibitor treatment. By analyzing the genetic and molecular profiles of individual tumors, healthcare providers can determine whether ARRY-424704 is a suitable treatment option for a specific patient, potentially improving treatment outcomes and reducing side effects.

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

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

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.