Selumetinib ≥95% (durch HPLC)

Lieferant: ENZO LIFE SCIENCES

Synonyme: 5-((4-Bromo-2-chlorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide, AZD6244

ENZCHM1840050
ENZOENZCHM1840050EA 158 EUR
ENZOENZCHM1840050
Selumetinib ≥95% (durch HPLC)
Selumetinib

Potent and selective ATP non-competitive inhibitor of MEK1/2


Selumetinib (AZD6244) is a second-generation, orally available, potent and selective ATP non-competitive inhibitor of MEK 1/2. In direct assays, AZD6244 selectively inhibits purified active MEK1 and MEK2 with an IC50 of 14 nM, and AZD6244 has reported IC50 values of <100nm for MEK1 in ELISA assays and in bindings assays against recombinant domains of MEK2, Kd values were 53nM for AZD6244. AZD6244 demonstrated very effective anti-proliferation effects against several different cell lines with IC50 values ranging from a low of 3nM to < 1 µM depending upon the cell system used, and the compound inhibits basal and growth factor-stimulated phosphorylation of ERK1/ 2 with IC50 concentrations < 40 nM. AZD6244 has demonstrated potent dose-dependent antitumor activity against a panel of mouse xenograft models of colorectal, pancreatic, liver, skin, and lung cancer, and inhibition of tumor growth was found to correlate with the reduction of phospho-ERK1/2 levels in tumors.

Formel: C₁₇H₁₅BrClFN₄O₃
Molecular Weight: 457,7 g/mol
MDL: MFCD11977472
CAS-Nummer: 606143-52-6
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