Selumetinib sulfate - 10mM in DMSO , Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor, CAS No.943332-08-9, Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor

CAS: 943332-08-9 Cat. No.: S656317 Molecular Weight: 555.76 EC Number: 642-432-8 PubChem CID: 16214875

GRADE & PURITY 10mM in DMSO

Storage

Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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.

Specifications

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

Desiccated, Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Mechanism of action

Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor

Names and Identifiers

• Isomeric SMILES: CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO.OS(=O)(=O)O
• Alternate CAS: 943332-08-9
• PubChem CID: 16214875
• NSC Number: 748727
• Molecular Weight: 555.76