Chemical Property of 4-methyl-3-(2-((2-morpholinoethyl)amino)quinazolin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzamide
Chemical Property:
- PKA:13.23±0.70(Predicted)
- PSA：86.10000
- Density:1.324
- LogP:5.36420
- Solubility.:Soluble in DMSO
- XLogP3:5.2
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:9
- Rotatable Bond Count:7
- Exact Mass:535.21950964
- Heavy Atom Count:39
- Complexity:795
- Purity/Quality:
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99%, *data from raw suppliers
AMG-47a *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)C3=CC4=CN=C(N=C4C=C3)NCCN5CCOCC5
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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.
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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.
