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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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 603.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.66 mL||8.28 mL||16.57 mL|
|5 mM||0.33 mL||1.66 mL||3.31 mL|
|10 mM||0.17 mL||0.83 mL||1.66 mL|
|50 mM||0.03 mL||0.17 mL||0.33 mL|
References are publications that support the biological activity of the product.
Johnson et al (2007) Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg.Med.Chem.Lett. 17 3339 PMID: 17448658
Walser et al (2006) Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer. Cancer Res. 66 7701 PMID: 16885372
Cambien et al (2009) Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism. Br.J.Cancer 100 1755 PMID: 19436305
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Keywords: (±)-AMG 487, (±)-AMG 487 supplier, CXCR3, chemokine, receptors, antagonists, inhibitors, inhibits, cell, migration, metastasis, ±-AMG487, ±-AMG_487, Chemokine, CXC, Receptors, 4487, Tocris Bioscience
2 Citations for (±)-AMG 487
Citations are publications that use Tocris products. Selected citations for (±)-AMG 487 include:
Gordón-Alonso et al (2017) Galectin-3 captures IF.-gamma in the tumor matrix reducing chemokine gradient production and T-cell tumor infiltration. Nat Commun 8 793 PMID: 28986561
Guo et al (2018) Interleukin-1β induces CXCR3-mediated chemotaxis to promote umbilical cord mesenchymal stem cell transendothelial migration. Stem Cell Res Ther. 9 281 PMID: 30359318
Do you know of a great paper that uses (±)-AMG 487 from Tocris? Please let us know.
Reviews for (±)-AMG 487
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.
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