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| | AMG-47a Basic information |
| Product Name: | AMG-47a | | Synonyms: | AMG-47a;AMG-47;4-Methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]benzamide;4-Methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]benzamide AMG-47A;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;AMG47A; GENETICIN;CS-1025 | | CAS: | 882663-88-9 | | MF: | C29H28F3N5O2 | | MW: | 535.56 | | EINECS: | | | Product Categories: | APIs | | Mol File: | 882663-88-9.mol |  |
| | AMG-47a Chemical Properties |
| 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 |
| | AMG-47a Usage And Synthesis |
| 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. |
| | AMG-47a Preparation Products And Raw materials |
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