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 a 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
- 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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Average Rating: 4 (Based on 1 Review)
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I used this product to reduce the activated CXCR3+ T cells in mouse with chronic interstitial cystitis.