Selumetinib sulfate - 10mM in DMSO, high purity , CAS No.943332-08-9(DMSO)

Item Number

S656317

• Specifications & Purity: 10mM in DMSO
• Biochemical and Physiological Mechanisms: Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC 50 of 14 nM for MEK1 . Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
• Storage Temp: Desiccated,Store at -80°C
• Shipped In: Ice chest + Ice pads

Product Description

Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC 50 of 14 nM for MEK1 . Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.