SAR131675

  Cat. No.:  DC8530   Featured
Chemical Structure
1433953-83-3
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More than 5000 active chemicals with high quality for research!
Field of application
SAR131675 is a potent and selective VEGFR-3 inhibitor.
Cas No.: 1433953-83-3
Chemical Name: SAR131675
Synonyms: SAR 131675;1,SAR-131675
SMILES: COC[C@](C#CC1C=CC2C(C(=C(N(CC)C=2N=1)N)C(NC)=O)=O)(C)O
Formula: C18H22N4O4
M.Wt: 358.391684055328
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM.
In Vivo: SAR131675 is very well tolerated in mice and shows a potent antitumoral effect in several orthotopic and syngenic models, including mammary 4T1 carcinoma and RIP1.Tag2 tumors. Interestingly, it significantly reduces lymph node invasion and lung metastasis, showing its antilymphangiogenic activity in vivo. SAR131675 significantly reduces TAM infiltration and aggregation in 4T1 tumors[1].
In Vitro: AR131675 is highly selective for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. However, it is moderately active on VEGFR-2 with a VEGFR-3/VEGFR-2 ratio of about 10. SAR131675 inhibits VEGFR-3 tyrosine kinase activity and VEGFR-3 autophosphorylation in HEK cells with IC50 values of 20 and 45 nM, respectively. 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. SSAR131675 has 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[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC9586 Telatinib Telatinib(Bay 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.
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DC3146 Sunitinib malate Sunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.
DC9781 SU4312(NSC86429) SU4312(NSC86429) is a selective, cell-permeable inhibitor of VEGFR2 and PDGFR tyrosine kinases (IC50s = 0.8 and 19.4 μM, respectively).
DC7509 SU1498 SU1498 is a selective inhibitor of the VEGFR2; inhibits Flk-1with an IC50 of value of 700 nM.
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