SAR131675 is a potent and selective VEGFR3 inhibitor with IC50 of 23 nM. SAR131675 is highly selective for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases, and is moderately active on VEGFR-2. 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 IC50 of 20 nM. SAR131675 significantly reduces lymph node invasion and lung metastasis, exhibits antilymphangiogenic activity in vivo, significantly reduces TAM infiltration and aggregation in 4T1 tumors.
Physicochemical Properties
M.Wt
358.39
Formula
C18H22N4O4
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Month
Shipping
Solubility
Chemical Name/SMILES
References
1. Alam A, et al. Mol Cancer Ther. 2012 Aug;11(8):1637-49.
2. Hwang SD, et al. Cell Death Dis. 2019 Mar 4;10(3):219.
