中文名 | AMG 487 |
英文名 | AMG 487 |
别名 | 化合物AMG 487 |
英文别名 | AMG 487 N-[(1R)-1-[3-(4-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)benzeneacetamide Benzeneacetamide, N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)- |
CAS | 473719-41-4 |
化学式 | C32H28F3N5O4 |
分子量 | 603.59 |
熔点 | 161.2℃ (ethyl acetate heptane ) |
溶解度 | DMSO : ≥ 41 mg/mL (67.93 mM)H2O : < 0.1 mg/mL (不溶) |
存储条件 | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
参考资料 展开查看 | 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. |
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 |
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