882663-88-9

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
• CAS NO: 882663-88-9
• Molecular Formula: C29H28F3N5O2
• Molecular Weight: 535.5601296
• Product Categories: APIs
• Mol File: 882663-88-9.mol
• Article Data: 2

Chemical Properties

• Appearance: /
• Density: 1.324
• Solubility: Soluble in DMSO
• PKA: 13.23±0.70(Predicted)
• CAS DataBase Reference: AMG-47a(CAS DataBase Reference)
• NIST Chemistry Reference: AMG-47a(882663-88-9)
• EPA Substance Registry System: AMG-47a(882663-88-9)

Safety Data

• Hazardous Substances Data: 882663-88-9(Hazardous Substances Data)

Usage

Description

AMG-47a is an orally bioavailable inhibitor of Lck, VEGF receptor 2 (VEGFR2/KDR), p38α, and JAK3, with IC50s of 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, but does inhibit Src (IC50 = 2 nM). AMG-47a has anti-inflammatory activity, decreasing IL-2 production induced by an anti-CD3 antibody in mice and inhibiting T cell proliferation in vitro.
Used in Pharmaceutical Industry:
AMG-47a is used as an inhibitor of lymphocyte-specific kinase (Lck) for its potential therapeutic applications in treating inflammatory and immune-related disorders. Its ability to decrease IL-2 production and inhibit T cell proliferation makes it a promising candidate for modulating immune responses.
Used in Oncology Research:
AMG-47a is used as a research tool for studying the role of Lck, VEGFR2, p38α, and JAK3 in cancer cell growth and proliferation. Its inhibitory effects on these kinases can provide insights into the development of targeted therapies for various types of cancer.
Used in Immunology Research:
AMG-47a is used as a research tool for investigating the role of Lck in T cell activation and immune responses. Its ability to inhibit T cell proliferation in vitro can help researchers understand the mechanisms of T cell regulation and develop new strategies for modulating immune responses.
Used in Drug Discovery and Development:
AMG-47a is used as a lead compound in the development of new drugs targeting Lck and other kinases involved in inflammatory and immune-related disorders. Its selectivity and potency make it a valuable starting point for designing more effective and targeted therapeutic agents.

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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Relevant articles and documents

Aryl nitrogen-containing bicyclic compounds and methods of use

The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, As