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(±)-AMG 487

Catalog #: 4487
5 Citations Datasheet / COA / SDS
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4487/10
4487/50
(±)-AMG 487 | CAS No. 947536-03-0 | Chemokine Receptor Antagonists
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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%

Product Details
Citations (5)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

(±)-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.

Technical Data

M.Wt:
603.59
Formula:
C32H28F3N5O4
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
947536-03-0

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.

Additional Information

Other Product-Specific Information:
  • This compound is racemic

Background References

  1. NF-?B signaling regulates cell-autonomous regulation of CXCL10 in breast cancer 4T1 cells
    WJ Jin, B Kim, D Kim, HY Park Choo, HH Kim, H Ha, ZH Lee
    Exp. Mol. Med, 2017;49(2):e295.
  2. Langerhans cells and NK cells cooperate in the inhibition of chemical skin carcinogenesis
    D Ortner, CH Tripp, K Komenda, S Dubrac, B Zelger, M Hermann, W Doppler, PZ Tymoszuk, L Boon, BE Clausen, P Stoitzner
    Oncoimmunology, 2017;6(2):e1260215.
  3. CXCL4 and CXCL4L1 Differentially Affect Monocyte Survival and Dendritic Cell Differentiation and Phagocytosis

    PLoS ONE, 2016;11(11):e0166006.
  4. Platelet factor 4 promotes rapid replication and propagation of Dengue and Japanese encephalitis viruses
    A Ojha, A Bhasym, S Mukherjee, GK Annarapu, T Bhakuni, I Akbar, T Seth, NK Vikram, S Vrati, A Basu, S Bhattachar, P Guchhait
    EBioMedicine, 2019;39(0):332-347.
  5. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
    Johnson et al.
    Bioorg.Med.Chem.Lett., 2007;17:3339
  6. Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer.
    Walser et al.
    Cancer Res., 2006;66:7701
  7. Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism.
    Cambien et al.
    Br.J.Cancer, 2009;100:1755

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Citations for (±)-AMG 487

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

5 Citations: Showing 1 - 5

  1. Wnt signaling enhances macrophage responses to IL-4 and promotes resolution of atherosclerosis.
    Authors: Hitoo Et al.
    Elife  2021;10
  2. Metastasis-initiating cells induce and exploit a fibroblast niche to fuel malignant colonization of the lungs.
    Authors: Tsunaki Et al.
    Nat Commun  2020;11:1494
  3. Neutrophils promote CXCR3-dependent itch in the development of atopic dermatitis.
    Authors: Karsten Et al.
    Elife  2019;8
  4. Interleukin-1β induces CXCR3-mediated chemotaxis to promote umbilical cord mesenchymal stem cell transendothelial migration.
    Authors: Guo Et al.
    Stem Cell Res Ther.  2018;9:281
  5. Galectin-3 captures IF.-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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