882663-88-9

882663-88-9 structure

Name: AMG-47a
Chemical Name: 4-methyl-3-[2-(2-morpholin-4-ylethylamino)quinazolin-6-yl]-N-[3-(trifluoromethyl)phenyl]benzamide
CAS Number: 882663-88-9
Molecular Formula: C₂₉H₂₈F₃N₅O₂
Molecular Weight: 535.560
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Src
Create Date: 2016-08-16 22:11:24
Modify Date: 2024-01-02 08:14:47
AMG-47a is a potent inhibitor of Lck and T cell proliferation; exhibits anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.IC50 value: Target: Lck inhibitorIn several other in vitro assays, AMG-47a displays subnanomolar inhibition against Lck, and low (<10 nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK α (p38α). In addition, at slightly higher doses but well under 10 μM, AMG-47a effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 μM. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.

Name	4-methyl-3-[2-(2-morpholin-4-ylethylamino)quinazolin-6-yl]-N-[3-(trifluoromethyl)phenyl]benzamide
Synonyms	4-Methyl-3-(2-{[2-(4-morpholinyl)ethyl]amino}-6-quinazolinyl)-N-[3-(trifluoromethyl)phenyl]benzamide 4-methyl-3-(2-{[2-(morpholin-4-yl)ethyl]amino}quinazolin-6-yl)-N-[3-(trifluoromethyl)phenyl]benzamide AMG-47a AMG-47 Benzamide, 4-methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]-

Description	AMG-47a is a potent inhibitor of Lck and T cell proliferation; exhibits anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.IC50 value: Target: Lck inhibitorIn several other in vitro assays, AMG-47a displays subnanomolar inhibition against Lck, and low (<10 nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK α (p38α). In addition, at slightly higher doses but well under 10 μM, AMG-47a effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 μM. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src Research Areas >> Inflammation/Immunology
References	[1]. Carver J, et al. A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein. PLoS One. 2014 Aug 5;9(8):e103836.