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Submit Review(±)-AMG 487
Description: CXCR3 antagonist; inhibits cell migration and metastasis
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
Purity: ≥98% (HPLC)
Biological Activity for (±)-AMG 487
(±)-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.
Compound Libraries for (±)-AMG 487
(±)-AMG 487 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for (±)-AMG 487
| M. Wt | 603.59 |
| Formula | C32H28F3N5O4 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 947536-03-0 |
| PubChem ID | 10282265 |
| InChI Key | WQTKNBPCJKRYPA-UHFFFAOYSA-N |
| Smiles | CCOC(C=C3)=CC=C3N2C(C1=CC=CN=C1N=C2C(N(CC4=CC=CN=C4)C(CC5=CC=C(OC(F)(F)F)C=C5)=O)C)=O |
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.
Solubility Data for (±)-AMG 487
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 60.36 | 100 |
Preparing Stock Solutions for (±)-AMG 487
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 |
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Product Datasheets for (±)-AMG 487
References for (±)-AMG 487
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
If you know of a relevant reference for (±)-AMG 487, please let us know.
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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
5 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
Hitoo et al (2021) Wnt signaling enhances macrophage responses to IL-4 and promotes resolution of atherosclerosis. Elife 10 PMID: 33720008
Karsten et al (2019) Neutrophils promote CXCR3-dependent itch in the development of atopic dermatitis. Elife 8 PMID: 31631836
Tsunaki et al (2020) Metastasis-initiating cells induce and exploit a fibroblast niche to fuel malignant colonization of the lungs. Nat Commun 11 1494 PMID: 32198421
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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AMG 487 reduces the symptoms and inflammation in interstitial cystitis..
By
Udai Singh on 01/04/2018
Assay Type: In Vivo
Species: Mouse
I used this product to reduce the activated CXCR3+ T cells in mouse with chronic interstitial cystitis.
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