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AZD6244 (Selumetinib,ARRY-142886) — Datasheet

CAT. NO. DC1069

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ParameterValue
Chemical NameSelumetinib
CAS No.606143-52-6
SynonymsAZD 6244;5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide;Selumetinib;Selumetinib (AZD6244);1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2- hydroxyethoxy)-1-methyl-;5-(4-bromo-2-chlorophenylamino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-c...;6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide;AZD-6244;AZD6244 (Selumetinib);Name: AZD 6244;SeluMetinib (AZD-6244);Selumetinib(AZD6244,ARRY-142886);6-(4-bromo-2-chlorophenylamino)-7-fluoro-N-(2-hydroxyethoxy)-3-methyl-3H-benzo[d]imidazole-5-carboxamide;Array142886;ARRY 142886;ARRY-142886;AZD6244;AZD6244(Selumetinib);5-((4-bromo-2-chlorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide;5-(4-broMo-2-chlorophenylaMino)-4-fluoro-N-(2-hydroxyethoxy)-1-Methyl-1H-benzo[d]iMidazole-6-carboxaMide
FormulaC17H15BrClFN4O3
M.Wt457.6814
SMILESBrC1C([H])=C([H])C(=C(C=1[H])Cl)N([H])C1=C(C2=C(C([H])=C1C(N([H])OC([H])([H])C([H])([H])O[H])=O)N(C([H])([H])[H])C([H])=N2)F
Purity98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Selumetinib is a highly potent MEK inhibitor, with an IC50 of 14 nM against MEK1.

In Vitro

Selumetinib causes a time- and dose-dependent reduction in DNA synthesis and cell viability in primary, induces growth arrest and apoptosis associated with the inactivation of ERK in primary 2-1318 cells[1]. Selumetinib (1µM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells[2]. Selumetinib (ARRY-142886) results in the growth inhibition of several cell lines containing B-Raf and Ras mutations but has no effect on a normal fibroblast cell line[3].

In Vivo

Selumetinib (AZD6244, 50 and 100 mg/kg, p.o.) decreases the growth rate of 4-1318 xenografts in a dose-dependent manner; AZD6244 when given at the dose of 50 mg/kg also significantly suppresses the growth of the 5-1318, 2-1318, 26-1004, and 29-1104 xenografts[1]. Selumetinib (ARRY-142886, 10, 25, 50, or 100 mg/kg, p.o.) is capable of inhibiting both ERK1/2 phosphorylation and growth of HT-29 xenograft tumors in nude mice. Tumor regressions are also seen in a BxPC3 xenograft model[3].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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