AMG 487

AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively[1].

Product Specifications

CAS Number

[473719-41-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

CXCR

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

Cancer-programmed cell death

Field of Research

Cancer; Inflammation/Immunology; Endocrinology

Assay Protocol

https://www.medchemexpress.com/AMG-487.html

Purity

99.80

Solubility

DMSO : ≥ 41 mg/mL

Smiles

O=C(N([C@@H](C1=NC2=NC=CC=C2C(N1C3=CC=C(OCC)C=C3)=O)C)CC4=CC=CN=C4)CC5=CC=C(OC(F)(F)F)C=C5

Molecular Formula

C32H28F3N5O4

Molecular Weight

603.59

Precautions

H302, H315, H319, H335

References & Citations

[1]Johnson M, et al. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2007 Jun 15;17 (12) :3339-43.|[2]Walser TC, et al. Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer. Cancer Res. 2006 Aug 1;66 (15) :7701-7.|[3]Cambien B, et al. Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism. Br J Cancer. 2009 Jun 2;100 (11) :1755-64.