AMG-47a

AMG-47a is an orally active, ATP-competitive Lck inhibitor (IC50=0.2 nM) . AMG-47a inhibits VEGF2, p38α, p38α, Jak3, MLR, and IL-2 with IC50 of 1 nM, 3 nM, 72 nM, 30 nM, and 21 nM, respectively. AMG-47a reduces T cell activation and the production of cytokines such as TGF-β, exerting anti-inflammatory and anti-fibrotic activities. AMG-47a can be used in the research of autoimmune diseases, pulmonary fibrosis, and KRAS mutation-associated cancers[1][2][3].

Product Specifications

CAS Number

[882663-88-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

JAK; p38 MAPK; Src; VEGFR

Type

Reference compound

Related Pathways

Epigenetics; JAK/STAT Signaling; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/AMG-47a.html

Purity

99.19

Solubility

DMSO : ≥ 34 mg/mL

Smiles

O=C(NC1=CC=CC(C(F)(F)F)=C1)C2=CC=C(C)C(C3=CC4=CN=C(NCCN5CCOCC5)N=C4C=C3)=C2

Molecular Formula

C29H28F3N5O2

Molecular Weight

535.56

Precautions

H302, H315, H319, H335

References & Citations

[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.|[2]DiMauro EF, et al. Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. J Med Chem. 2006 Sep 21;49 (19) :5671-86.|[3]Kagawa K, et al. The lymphocyte-specific protein tyrosine kinase-specific inhibitor A-770041 attenuates lung fibrosis via the suppression of TGF-β production in regulatory T-cells. PLoS One. 2022 Oct 27;17 (10) :e0275987.