(±)-AMG 487

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Cat.No. 4487 - (±)-AMG 487 | C32H28F3N5O4 | CAS No. 947536-03-0
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)
Datasheet
Citations (1)
Reviews (1)
Literature

Biological Activity

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

(±)-AMG 487 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 60.36 100

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 solvent 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

Certificate of Analysis / Product Datasheet
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References

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

1 Citation for (±)-AMG 487

Citations are publications that use Tocris products. Selected citations for (±)-AMG 487 include:

Gordón-Alonso et al (2017) Galectin-3 captures interferon-gamma in the tumor matrix reducing chemokine gradient production and T-cell tumor infiltration. Nat Commun 8 793 PMID: 28986561


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Reviews for (±)-AMG 487

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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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