AMG 487
AMG 487
CAS: 473719-41-4
Molecular Formula: C32H28F3N5O4
AMG 487 - Names and Identifiers
AMG 487 - Physico-chemical Properties
| Molecular Formula | C32H28F3N5O4 |
| Molar Mass | 603.59 |
| Melting Point | 161.2℃ (ethyl acetate heptane ) |
| Solubility | DMSO : ≥ 41 mg/mL (67.93 mM)H2O : < 0.1 mg/mL (insoluble) |
| Storage Condition | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| Use | AMG 487 is an effective, orally active and selective chemokine receptor 3 (CXCR3) antagonist. IC50 values for inhibiting CXCL10 and CXCL11 binding to CXCR3 are 8.0 and 8.2 nM respectively. |
AMG 487 - Reference
| Reference Show more | 1: Henne KR, Tran TB, VandenBrink BM, Rock DA, Aidasani DK, Subramanian R, Mason AK, Stresser DM, Teffera Y, Wong SG, Johnson MG, Chen X, Tonn GR, Wong BK. Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. Drug Metab Dispos. 2012 Jul;40(7):1429-40. doi: 10.1124/dmd.112.045708. Epub 2012 Apr 19. PubMed PMID: 22517972. 2: Laragione T, Brenner M, Sherry B, Gulko PS. CXCL10 and its receptor CXCR3 regulate synovial fibroblast invasion in rheumatoid arthritis. Arthritis Rheum. 2011 Nov;63(11):3274-83. doi: 10.1002/art.30573. PubMed PMID: 21811993; PubMed Central PMCID: PMC3205193. 3: Liu J, Fu Z, Li AR, Johnson M, Zhu L, Marcus A, Danao J, Sullivan T, Tonn G, Collins T, Medina J. Optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5114-8. doi: 10.1016/j.bmcl.2009.07.032. Epub 2009 Jul 10. PubMed PMID: 19632842. 4: Pradelli E, Karimdjee-Soilihi B, Michiels JF, Ricci JE, Millet MA, Vandenbos F, Sullivan TJ, Collins TL, Johnson MG, Medina JC, Kleinerman ES, Schmid-Alliana A, Schmid-Antomarchi H. Antagonism of chemokine receptor CXCR3 inhibits osteosarcoma metastasis to lungs. Int J Cancer. 2009 Dec 1;125(11):2586-94. doi: 10.1002/ijc.24665. PubMed PMID: 19544560; PubMed Central PMCID: PMC2772145. |
AMG 487 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.657 ml | 8.284 ml | 16.568 ml |
| 5 mM | 0.331 ml | 1.657 ml | 3.314 ml |
| 10 mM | 0.166 ml | 0.828 ml | 1.657 ml |
| 5 mM | 0.033 ml | 0.166 ml | 0.331 ml |
Last Update：2024-01-02 23:10:35
AMG 487 - Reference Information
| biological activity | AMG 487 is an orally active, selective antagonist of CXC chemokine receptor 3 (CXCR3), it inhibited the binding of CXCR3 by IP-10 (CXCL10) and ITAC (CXCL11), corresponding to IC50 values of 8.0 nM and 8.2 nM, respectively. |
| Target | Value |
| CXCR3-CXCL10 (Cell-free assay) | 8.0 nM |
| CXCR3-CXCL11 (Cell-free assay) | 8.2 nM |
Last Update：2024-04-09 20:52:54
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Product Name: AMG 487 Visit Supplier Webpage Request for quotationCAS: 473719-41-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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