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MEK162 (ARRY-162, ARRY-438162)
Cat No.
CEI-1418
Description
MEK162 is a potent inhibitor of MEK1/2 with IC50 value of 12 nM.
Product Overview
MEK162 (ARRY-162, ARRY-438162) is a novel, selective inhibitor of MEK 1/2 with IC50 of about 12 nM. Co-treatment of MEK162 and PKC inhibitors persistently inhibited MAP-kinase pathway. The co-treatment can halt proliferation and induce apoptosis of uveal melanoma cells even with GNAQ or GNA11 mutations. All N-RAS mutant melanoma cells were sensitive to MEK 162.MEK162 reduced ERK1/2 phosphorylation, clonogenic survival, and induced apoptosis. Phase Ib or II clinical trials were conducted in 32 cutaneous melanoma patients. 20 patients in MEK162 monotherapy and 12 on MEK162 plus RAF inhibitor or selective BRAF inhibitor combination therapy underwent ophthalmological examinations and multimodal imaging. Thesetherapy all induced transient retinopathy with multiple bilateral lesions in some patients. The effect of MEK162 in retinopathy has been usually mild, self-limiting, and tolerable
CAS No.
606143-89-9
Molecular Weight
441.23
Purity
0.9802
Storage
Store at -20°C
Targets
MEK1; MEK2
IC50
12 nM; 12 nM
Molecular Formula
C17H15BrF2N4O3
Chemical Name
6-(4-bromo-2-fluoroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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