Selumetinib (AZD6244) , ≥99% , 606143-52-6

CAS NO.：606143-52-6

Empirical Formula: C17H15BrClFN4O3

Molecular Weight: 457.68

MDL number: MFCD11977472

EINECS: 207-313-3

PRODUCT Properties

• Melting point: >219°C (dec.)
• Density: 1.69
• storage temp.: -20°
• solubility: Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 2 mg/ml)
• form: Beige powder.
• pka: 14.20±0.10(Predicted)
• color: White
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.

Description and Uses

Selumetinib (AZD6244; ARRY-142886) is an oral MEK inhibitor. In a randomized trial, NSCLC patients with wild-type KRAS were randomized to erlotinib alone or combination therapy with selumetinib, while mutant KRAS patients were randomized to selumetinib alone or combination therapy. The primary end points were PFS for the KRAS wild-type cohort and objective response rate (ORR) for the KRAS mutant cohort. Results were not impressive, with no PFS difference in the KRAS wild-type arm (2.4 vs. 2.1?months) and no ORR difference in the KRASmutated subgroup (0% vs. 10%). A planned trial of selumetinib in combination with the anti-PD-L1 antibody durvalumab has since been suspended (NCT03004105).

It is a tight-binding, uncompetitive inhibitor of mitogen-activated protein kinase kinases (MEK) 1 and 2 currently in clinical development. It is useful as biomarker in human lung cancer cell. Potent MEK inhibitor.

Safety

• Symbol(GHS): GHS05,GHS07,GHS08
• Signal word: Danger
• Hazard statements: H317-H318-H361d-H373
• Precautionary statements: P262-P280-P312
• HS Code: 29349990