AMG 47a – 50 mg

Brand:
Cayman
CAS:
882663-88-9
Storage:
-20
UN-No:
Non-Hazardous - /

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).{39861} 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.{39862}  

 

Available on backorder

SKU: 25339 - 50 mg Category:

Description

A multi-kinase inhibitor; inhibits Lck, VEGFR2/KDR, p38α, and JAK3 (IC50s = 0.2, 1, 3, and 72 nM, respectively); 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); inhibits T cell proliferation in vitro in a mixed lymphocyte reaction assay (IC50 = 30 nM); decreases production of IL-2 induced by an anti-CD3 antibody in mice at 10, 30, and 100 mg/kg; decreases levels of mutant oncogene KRASG12V in HeLa cells in a reporter assay at 1 µM


Formal name: 4-methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]-benzamide

Synonyms: 

Molecular weight: 535.6

CAS: 882663-88-9

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Kinase Inhibitors|p38 MAPK||Product Type|Biochemicals|Kinase Inhibitors|SRC Family||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cancer|Cell Signaling|p38 MAPK Signaling||Research Area|Immunology & Inflammation|Adaptive Immunity