Selumetinib is a highly potent MEK inhibitor, with an IC50 value of 14 nM against MEK1.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. Selumetinib (1µM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells. 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.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.
MEK Inhibitor Related Products:
Mirdametinib (PD0325901); Trametinib; PD184352 (CI-1040); PD98059; BIX02189; U0126-EtOH; Pimasertib; BIX02188; TAK-733; Binimetinib (MEK162); SL327; Refametinib; GDC-0623; RO5126766 (CH5126766); Cobimetinib; APS-2-79 hydrochloride; AZD8330