| Identification | Back Directory | [Name]
AMG-47a | [CAS]
882663-88-9 | [Synonyms]
AMG-47
AMG-47a
CS-1025
AMG47A; GENETICIN
AMG 47;AMG-47;AMG47
4-Methyl-3-(2-((2-morpholinoethyl)amino)quinazolin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzamid
4-methyl-3-(2-((2-morpholinoethyl)amino)quinazolin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzamide
4-methyl-3-[2-(2-morpholin-4-ylethylamino)quinazolin-6-yl]-N-[3-(trifluoromethyl)phenyl]benzamide
4-Methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]benzamide
Benzamide, 4-methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]-
4-Methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]benzamide AMG-47A | [Molecular Formula]
C29H28F3N5O2 | [MDL Number]
MFCD09970318 | [MOL File]
882663-88-9.mol | [Molecular Weight]
535.56 |
| Chemical Properties | Back Directory | [density ]
1.324 | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Powder | [pka]
13.23±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
AMG 47a is an orally bioavailable inhibitor of Lck, VEGF receptor 2 (VEGFR2/KDR), p38α, and JAK3 (IC50s = 0.2, 1, 3, and 72 nM, respectively). It is selective for these kinases over a panel of additional kinases including SYK, JNK1, and PKAβ (IC50s = 292 to >25,000 nM) but does inhibit Src (IC50 = 2 nM). It decreases IL-2, but not TNF-α, 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. | [Uses]
AMG-47a is a inhibitor of lymphocyte-specific kinase (Lck), which is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and natural killer (NK) cells. | [References]
1. carver j, dexheimer ts, hsu d et al. a high-throughput assay for small molecule destabilizers of the krasoncoprotein. plos one. 2014 aug 5;9(8):e103836. |
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