AMG 47a

AMG 47a

CAT N°: 25339
Price:

From 182.00 154.70

AMG 47a is an orally bioavailable inhibitor of Lck, VEGF receptor 2 (VEGFR2/KDR), p38?, and JAK3 (IC50s = 0.2, 1, 3, and 72 nM, respectively).{39861} It is selective for these kinases over a panel of additional kinases including SYK, JNK1, and PKA? (IC50s = 292 to >25,000 nM) but does inhibit Src (IC50 = 2 nM). It decreases IL-2, but not TNF-?, production induced by an anti-CD3 antibody in 50% whole blood and inhibits T cell proliferation in vitro in a mixed lymphocyte reaction assay (IC50 = 30 nM). AMG 47a (10, 30, and 100 mg/kg) has anti-inflammatory activity, decreasing production of IL-2 induced by an anti-CD3 antibody in mice. It also decreases levels of mutant oncogene KRASG12V in HeLa cells in a reporter assay when used at a concentration of 1 µM.{39862}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 4-methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]-benzamide
  • Correlated keywords
    • AMG47a AMG47-a 47 multikinase VEGFR-2 p38-? p-38? p JAK-3 JNK-1 PKA-? IL2 TNF? antiCD-3 antiCD3 antiinflammatory body
  • Product Overview:
    AMG 47a is an orally bioavailable inhibitor of Lck, VEGF receptor 2 (VEGFR2/KDR), p38?, and JAK3 (IC50s = 0.2, 1, 3, and 72 nM, respectively).{39861} It is selective for these kinases over a panel of additional kinases including SYK, JNK1, and PKA? (IC50s = 292 to >25,000 nM) but does inhibit Src (IC50 = 2 nM). It decreases IL-2, but not TNF-?, production induced by an anti-CD3 antibody in 50% whole blood and inhibits T cell proliferation in vitro in a mixed lymphocyte reaction assay (IC50 = 30 nM). AMG 47a (10, 30, and 100 mg/kg) has anti-inflammatory activity, decreasing production of IL-2 induced by an anti-CD3 antibody in mice. It also decreases levels of mutant oncogene KRASG12V in HeLa cells in a reporter assay when used at a concentration of 1 µM.{39862}

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