SAR131675 is a selective inhibitor of VEGFR-3 with IC50 value of 20nM .
SAR131675 is an ATP-competitive inhibitor. It inhibits recombinant human VEGFR-3 with IC50 value of 23nM and inhibits the kinase activity of VEGFR-3 with Ki value of 12nM. SAR131675 is found to be cell permeable and inhibits VEGFR-3 autophosphorylation in HEK cells with IC50 values ranging from 30nM to 50nM. SAR131675 shows IC50 values of >3μM and 235nM against VEGFR-1 and VEGFR-2, respectively. It also havs no inhibitory effect on a panel of 65 kinases, 107 nonkinase enzymes and receptors and on 21 ion channels. Moreover, SAR131675 inhibits lymphatic cell survival induced by VEGFC and VEGFD with IC50 values of 14nM and 17nM. On another hand, SAR131675 exerts inhibition of the migration induced by VEGFA or VEGFC with IC50 values of 100nM and <30nM in HLMVEC cells, respectively .
In vivo, SAR131675 abrogates lymphangiogenesis and angiogenesis induced by FGF2. It also shows antitumor activity in the mice models. Treatment with SAR131675 significantly reduces the tumor volume of 4T1 mammary carcinoma tumors 
 Alam A, Blanc I, Gueguen-Dorbes G, et al. SAR131675, a Potent and Selective VEGFR-3–TK Inhibitor with Antilymphangiogenic, Antitumoral, and Antimetastatic Activities. Molecular cancer therapeutics, 2012, 11(8): 1637-1649.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥17.9mg/mL in DMSO|
|Canonical SMILES||CCN(C(N)=C1C(NC)=O)C2=NC(C#C[[email protected]](C)(COC)O)=CC=C2C1=O|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Description||SAR131675 is an inhibitor of VEGFR3 with IC50/Ki of 23 nM/12 nM, respectively.|
|IC50||23 nM (Ki=12 nM)|