SAR131675 - CAS 1433953-83-3
Catalog number: B0084-463427
Category: Inhibitor
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Molecular Formula:
C18H22N4O4
Molecular Weight:
358.39
COA:
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Targets:
VEGFR
Description:
SAR131675 dose dependently inhibits the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC50 of about 20 nM.
Purity:
>98%
Related CAS:
1092539-44-0
Appearance:
Solid powder
Synonyms:
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; SAR131675; SAR 131675; SAR-131675
MSDS:
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Canonical SMILES:
O=C(C(C(NC)=O)=C(N)N1CC)C2=C1N=C(C#CC(O)(COC)C)C=C2
1.Specific Inhibition of the VEGFR-3 Tyrosine Kinase by SAR131675 Reduces Peripheral and Tumor Associated Immunosuppressive Myeloid Cells.
Espagnolle N1, Barron P2, Mandron M3, Blanc I4, Bonnin J5, Agnel M6, Kerbelec E7, Herault JP8, Savi P9, Bono F10, Alam A11. Cancers (Basel). 2014 Feb 28;6(1):472-90. doi: 10.3390/cancers6010472.
Myeloid derived suppressor cells (MDSCs) and tumor-associated macrophages (TAMs) represent prominent components in cancer progression. We previously showed that inhibition of the VEGFR-3 pathway by SAR131675 leads to reduction of TAM infiltration and tumor growth. Here, we found that treatment with SAR131675 prevents the accumulation of immunosuppressive blood and splenic MDSCs which express VEGFR-3, in 4T1 tumor bearing mice. Moreover we showed that soluble factors secreted by tumor cells promote MDSCs proliferation and differentiation into M2 polarized F4/80+ macrophages. In addition, cell sorting and transcriptomic analysis of tumor infiltrating myeloid cells revealed the presence of a heterogeneous population that could be divided into 3 subpopulations: (i) immature cells with a MDSC phenotype (GR1+/CD11b+/F4/80-); (ii) "immuno-incompetent" macrophages (F4/80high/CD86neg/MHCIILow) strongly expressing M2 markers such as Legumain, CD206 and Mgl1/2 and (iii) "immuno-competent"-M1 like macrophages (F4/80Low/CD86+/MHCIIHigh).
2.SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities.
Alam A1, 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. Mol Cancer Ther. 2012 Aug;11(8):1637-49. doi: 10.1158/1535-7163.MCT-11-0866-T. Epub 2012 May 14.
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 dose dependently inhibited the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC(50) of about 20 nmol/L. SAR131675 was found to be highly selective for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. However, it was moderately active on VEGFR-2 with a VEGFR-3/VEGFR-2 ratio of about 10. SAR131675 had no antiproliferative activity on a panel of 30 tumors and primary cells, further showing its high specificity and indicating that SAR131675 is not a cytotoxic or cytostatic agent. SAR131675 was very well tolerated in mice and showed a potent antitumoral effect in several orthotopic and syngenic models, including mammary 4T1 carcinoma and RIP1.Tag2 tumors. Interestingly, it significantly reduced lymph node invasion and lung metastasis, showing its antilymphangiogenic activity in vivo.
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CAS 1433953-83-3 SAR131675

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