Selumetinib sulfate (AZD6244 sulfate) is an orally available, selective and potent MEK1/2 inhibitor that inhibits MEK1/2 phosphorylation and may be useful for the study of symptomatic refractory fibroids in type 1 neurofibromatosis.

purified MEK:12 nM

Selumetinib sulfate (AZD6244) is a potent MEK inhibitor with an IC50 of 12 nM for purified MEK.Selumetinib sulfate is able to inhibit ERK1/2 phosphorylation in a variety of cancer cell lines with IC50s as low as 8 nM, both at basal and induced levels. In primary 2-1318 cells, Selumetinib sulfate induces growth arrest and apoptosis associated with ERK inactivation, resulting in reduced primary DNA synthesis and reduced cell viability over time and dose. [1]
In H-441 and H-1437 cells, Selumetinib sulfate (1 μM) exhibits antiproliferative effects by blocking the G0/G1 phase. [2]
In addition, Selumetinib sulfate inhibited the growth of various cell lines harboring B-Raf and Ras mutations, but had no significant effect on normal fibroblast cell lines. [3]

In in vivo experiments, oral administration of 50 and 100 mg/kg Selumetinib sulfate dose-dependently reduced the growth rate of 4-1318 xenograft tumors; it also significantly inhibited the growth of 5-1318, 2-1318, 26-1004, and 29-1104 xenograft tumors at the 50 mg/kg dose. [1]
Oral administration of 10, 25, 50, or 100 mg/kg Selumetinib sulfate also inhibited ERK1/2 phosphorylation and reduced HT-29 xenograft tumor growth in nude mice. Meanwhile, tumor regression was observed in the BxPC3 xenograft model. [3]