Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :SAR1316751433953-83-3HY-158358.39C18H22N4O4>98%ySolubility:DMSO 30mg/mlgMechanisms: Pathways:Protein Tyrosine Kinase/RTK; Target:VEGFR Biological Activity:SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM, about 50- and 10-fold moreSAR131675isaVEGFR3inhibitorwithIC50/Kiof23nM/12nMabout50and10foldmoreselective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc. IC50 value: 23 nM [1] Target: VEGFR3 in vitro: VEGFR-3 ligands VEGFC and VEGFD, with an IC50 of about 20 nM. SAR131675 dosedependently inhibits rh-VEGFR-3–TK activity with an IC50 of 23 nM. SAR131675 inhibits VEGR-3–TK activity with a Ki of about 12 nM. SAR131675 inhibits VEGFR-1–TK activity with an IC50 of > 3 μyM and VEGFR-2–TK activity with an IC50 of 235 nM. SAR131675 inhibits VEGFR-1autophosphorylation with an IC50 of about 1 μM and VEGFR-2 with an IC50 of about 280 nM.SAR131675 moderately inhibits VEGFR-2 and has very little effect on VEGFR-1, showing a goodselectivity for VEGFR-3. SAR131675 inhibits VEGFA-induced VEGFR-2 phosphorylation in a dose-dependentmannerReferences:[1]. Alam A, Blanc I, Gueguen-Dorbes G, et al. SAR131675, a potent and selective VEGFR-3-TKinhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities. Mol Cancer Ther. 2012Aug;11(8):1637-49. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com 18 Wilkinson Way, Princeton, NJ 080,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr
