MEK162 (ARRY-162), MEK Inhibitor


Catalog No. size PriceQuantity
M60080-5S 5mg solid $119
M60080-50S 50mg solid $690

Description

Product Information
Molecular Weight: 441.23
Formula: C17H15BrF2N4O3
Purity: ≥ 98%
CAS#: 606143-89-9
Solubility: DMSO up to 100 mM
Chemical Name: 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

MEK162 (ARRY-162) is a highly potent, selective, and orally bioavailable MEK inhibitor. It is a non-ATP competitive inhibitor of MEK1/2 (IC50 ~ 12 nM). It can inhibit pERK (IC50 ~11 nM) in cellular assays. At up to 20 µM it has no activity against a panel of 220 other kinases. MEK162 is especially potent at inhibiting cell proliferation of mutant B-Raf and Ras cell lines, such as HT29, Malme-3M, SK-MEL-2, COLO 205, SK-MEL-28 and A375 (IC50 from 30-250 nM). In vivo it has demonstrated efficacy in several xenograft tumor models in mice, including HT29, BxPC3, MIA PaCa2, A549, LoVo, Calu6, DU145 and COLO 205. In the HT29 and in the COLO 205 colon carcinoma models, dose-dependent inhibition of tumor growth (up to 75% TGI) was observed at doses ranging from 3 to 30 mg/kg, QD, PO for 21 days. Currently a phase I study of MEK162 in patients with biliary tract cancer is undergoing. MEK162 also shows inhibition of cytokine production such as IL-1, TNF and IL-6 in clinical trials for patients with rheumatoid arthritis.

 

How to Use:

 

  • In vitro:  MEK162 was used at 1 µM final concentration in vitro and in cellular assays.
  • In vivo:   MEK162 was orally dosed to mice at 3-30 mg/kg once per day.

 

 

Reference: 




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