SAR131675
SAR131675 is a potent and selective VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity and VEGFR-3 autophosphorylation in HEK cells with IC(50) values of 20 and 45 nmol/L, respectively. SAR131675 was found to be highly selective for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is the first highly specific VEGFR-3-TK inhibitor described to date, displaying significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | SAR131675 |
|---|---|
| Iupac 化学名称 | 2-amino-1-ethyl-7-(3-hydroxy-4-methoxy-3-methylbut-1-yn-1-yl)-N-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide |
| 同义词 | SAR131675; SAR 131675; SAR-131675. |
| 英文同义词 | SAR131675; SAR 131675; SAR-131675. |
| 分子式 | C18H22N4O4 |
| 分子量 | 358.398 |
| Smile | O=C(C(C(NC)=O)=C(N)N1CC)C2=C1N=C(C#CC(O)(COC)C)C=C2 |
| InChiKey | PFMPOBVAYMTUOX-UHFFFAOYSA-N |
| InChi | InChI=1S/C18H22N4O4/c1-5-22-15(19)13(17(24)20-3)14(23)12-7-6-11(21-16(12)22)8-9-18(2,25)10-26-4/h6-7,25H,5,10,19H2,1-4H3,(H,20,24) |
| Cas号 | 1433953-83-3 |
| 相关CAS号 | 1433953-83-3 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 可溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Yu J, Mao L, Guan L, Zhang Y, Zhao J. Ginsenoside Rg1 enhances lymphatic transport of intrapulmonary silica via VEGF-C/VEGFR-3 signaling in silicotic rats. Biochem Biophys Res Commun. 2016 Mar 25;472(1):182-8. doi: 10.1016/j.bbrc.2016.02.091. Epub 2016 Feb 23. PubMed PMID: 26920056.
2: Bhuiyan MI, Kim JC, Hwang SN, Lee MY, Kim SY. Ischemic tolerance is associated with VEGF-C and VEGFR-3 signaling in the mouse hippocampus. Neuroscience. 2015 Apr 2;290:90-102. doi: 10.1016/j.neuroscience.2015.01.025. Epub 2015 Jan 28. PubMed PMID: 25637798.
3: Nihei M, Okazaki T, Ebihara S, Kobayashi M, Niu K, Gui P, Tamai T, Nukiwa T, Yamaya M, Kikuchi T, Nagatomi R, Ebihara T, Ichinose M. Chronic inflammation, lymphangiogenesis, and effect of an anti-VEGFR therapy in a mouse model and in human patients with aspiration pneumonia. J Pathol. 2015 Mar;235(4):632-45. doi: 10.1002/path.4473. Epub 2015 Jan 7. PubMed PMID: 25348279.
4: Osborn AJ, Dickie P, Neilson DE, Glaser K, Lynch KA, Gupta A, Dickie BH. Activating PIK3CA alleles and lymphangiogenic phenotype of lymphatic endothelial cells isolated from lymphatic malformations. Hum Mol Genet. 2015 Feb 15;24(4):926-38. doi: 10.1093/hmg/ddu505. Epub 2014 Oct 6. PubMed PMID: 25292196.
5: Espagnolle N, Barron P, Mandron M, Blanc I, Bonnin J, Agnel M, Kerbelec E, Herault JP, Savi P, Bono F, Alam A. Specific Inhibition of the VEGFR-3 Tyrosine Kinase by SAR131675 Reduces Peripheral and Tumor Associated Immunosuppressive Myeloid Cells. Cancers (Basel). 2014 Feb 28;6(1):472-90. doi: 10.3390/cancers6010472. PubMed PMID: 24589997; PubMed Central PMCID: PMC3980599.
6: Alam A, Blanc I, Gueguen-Dorbes G, Duclos O, Bonnin J, Barron P, Laplace MC, Morin G, Gaujarengues F, Dol F, Hérault JP, Schaeffer P, Savi P, Bono F. SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities. Mol Cancer Ther. 2012 Aug;11(8):1637-49. doi: 10.1158/1535-7163.MCT-11-0866-T. Epub 2012 May 14. PubMed PMID: 22584122.
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