Selumetinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效、选择性、ATP 非竞争性的 MEK1/2 抑制剂，MEK1 的 IC50/Ki 为 14.1 nM/22.6 nM。

A highly potent and selective, ATP-uncompetitive inhibitor of MEK1/2 with IC50/Ki of 14.1 nM/22.6 nM for MEK1; shows no activity against other 40 serine/threonine and tyrosine kinases; inhibits cellular ERK1/2 phosphorylation (IC50<40 nM), suppresses growth inhibition of several cell lines containing B-Raf and Ras mutations (IC50=59-473 nM); causes growth of HT-29 xenograft tumors in nude mice.Skin Cancer Approved(In Vitro):Selumetinib (AZD6244) 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.Selumetinib (AZD6244) (1μM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells.Selumetinib (AZD6244) 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.(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. 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.

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ARRY-142886 | AZD-6244

MAPK/ERK Signaling

MEK

MEK1

Cancer

Skin Cancer

606143-52-6

457.6814

C17H15BrClFN4O3

>98% (HPLC)

DMSO: ≥ 34 mg/mL

O=C(C1=C(NC2=CC=C(Br)C=C2Cl)C(F)=C3C(N(C)C=N3)=C1)NOCCO

1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-

(-20℃)

With Ice Pack

≥ 2 years