Chemical Name: N-1-[(3-4(-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)benzeneacetamide
Biological Activity(±)-AMG 487 is an antagonist of CXCR3; inhibits binding of 125I-IP-10 and 125I-ITAC to CXCR3 (IC50 values are 8.0 and 8.2 nM respectively). Inhibits CXCR3-mediated cell migration by the chemokines IP-10, ITAC and MiG in vitro (IC50 values are 8, 15 and 36 nM respectively). Also shown to inhibit lung metastasis in a mouse model of metastatic breast cancer.
This product is racemic.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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- This compound is racemic
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
Johnson et al.
Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer.
Walser et al.
Cancer Res., 2006;66:7701
Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism.
Cambien et al.
Citations for (±)-AMG 487
The citations listed below are publications that use Tocris products. Selected citations for (±)-AMG 487 include:
2 Citations: Showing 1 - 2
Interleukin-1β induces CXCR3-mediated chemotaxis to promote umbilical cord mesenchymal stem cell transendothelial migration.
Authors: Guo Et al.
Stem Cell Res Ther. 2018;9:281
Galectin-3 captures IF.-gamma in the tumor matrix reducing chemokine gradient production and T-cell tumor infiltration.
Authors: Gordón-Alonso Et al.
Nat Commun 2017;8:793
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