(±)-AMG 487

Name: (±)-AMG 487
Brand: Tocris Bioscience
SKU: 4487
Rating: 4 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 4487

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Citations (44)

COA / SDS

CXCR3 antagonist; inhibits cell migration and metastasis

Key Product Details

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)
Molecular Weight:	603.59

View Full Technical Details for (±)-AMG 487

Technical Data
Citations / Reviews (1)

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 for (±)-AMG 487

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for (±)-AMG 487

References are publications that support the biological activity of the product.

Walser Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer. Cancer Res. 2006 PMID: 16885372
Cambien Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism. Br.J.Cancer 2009 PMID: 19436305
Johnson Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg.Med.Chem.Lett. 2007 PMID: 17448658