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 ActivityAntagonist 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. All Tocris products are intended for laboratory research use only.
- 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.
Citation for (±)-AMG 487
The citations listed below are publications that use Tocris products. Selected citations for (±)-AMG 487 include:
1 Citation: Showing 1 - 1
Galectin-3 captures interferon-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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I used this product to reduce the activated CXCR3+ T cells in mouse with chronic interstitial cystitis.