SAR 131675
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.
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Chemical Information
| Name | SAR 131675 |
|---|---|
| Iupac Chemical Name | 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 |
| Synonyms | SAR131675; SAR 131675; SAR-131675. |
| Molecular Formula | C18H22N4O4 |
| Molecular Weight | 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 Number | 1433953-83-3 |
| Related CAS | 1433953-83-3 |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| 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.
Chemical Structure
-N-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide_1433953-83-3.png)