Molecular Weight(MW): 358.39
SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.
Cited by 7 Publications
2 Customer Reviews
Blockade of IPC-induced ischemic tolerance by the VEGFR-3 inhibitor SAR131675. (A) Representative images of FJ-stained brain sections from sham + SARH (i), sham-IPC + SI + Veh (ii), IPC + SI + Veh (iii) and IPC + SI + SARH (iv) groups. Note that there were more degenerated neurons in the IPC + SI + SARH group receiving SAR131675 of 50 mg/kg as an initial dose than in the IPC + SI + Veh group. Scale bar = 50 μm. (B) The quantitative analysis shows the number of FJ-positive degenerated neurons in the CA1 subregion of the different treatment groups including the IPC + SI + SARL group receiving SAR131675 of 25 mg/kg as an initial dose. Data are presented as the mean ± SEM; # p < 0.05 compared with the sham-IPC + SI + Veh group; *p < 0.05 compared with the IPC + SI + Veh group. (C) Representative images of NeuN immunofluorescence in the sham + SARH (i), sham-IPC + SI + Veh (ii), IPC + SI + Veh (iii) and IPC + SI + SARH (iv) groups. Note that NeuN-immunofluorescence in the IPC + SI + SARH group was reduced compared with the IPC + SI + Veh group. Scale bar = 50 μm. (D) The quantitative analysis shows the number of NeuN-positive intact pyramidal neurons in the CA1 subregion for the different treatment groups. Data are presented as the mean ± SEM; #p < 0.05 compared with the sham-IPC + SI + Veh group; *p < 0.05 compared with the IPC + SI + Veh group.
Neuroscience, 2015, 290C:90-102.. SAR131675 purchased from Selleck.
LYVE-1 expression further increases in the lung interstitium of silicosis model of rats after ginsenoside Rg1 treatment. (A) Staining of the lung interstitium of silicotic rats showed a significant expression of LYVE-1–positive lymphatic vessels (brown and arrows) in the Vehicle, Rg1 and Rg1+SAR131675 groups, but which was not seen in the Sham group.
Biochem Biophys Res Commun, 2016, 472(1):182-8.. SAR131675 purchased from Selleck.
Purity & Quality Control
Choose Selective VEGFR Inhibitors
|Description||SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.|
|Features||A potent and selective VEGFR-3–tyrosine kinase inhibitor.|
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. SAR131675 dose dependently 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 μM and VEGFR-2–TK activity with an IC50 of 235 nM. SAR131675 inhibits VEGFR-1 autophosphorylation 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 good selectivity for VEGFR-3. SAR131675 inhibits VEGFA-induced VEGFR-2 phosphorylation in a dose-dependent manner, with an IC50 of 239 nM. SAR131675 potently inhibits lymphatic cell survival induced by VEGFC and VEGFD with IC50 of 14 nM and 17 nM, respectively. SAR131675 inhibits VEGFA-induced survival with an IC50 of 664 nM. SAR131675, significantly and dose dependently inhibits VEGFC-induced Erk phosphorylation, with an IC50 of about 30 nM. 
|In vivo||In embryonic angiogenesis using the zebrafish model, SAR131675 efficiently impaires embryonic vasculogenesis. SAR131675 at 100 mg/kg/d has significantly reduced the levels of VEGFR-3 and hemoglobin content by about 50%. SAR131675 efficiently abrogates lymphangiogenesis and angiogenesis induced in vivo by FGF2. SAR131675 at a dose of 300 mg/kg is able to inhibit both VEGFR-2 and VEGFR-3 signaling. In the prevention study, 5 weeks treatment with SAR131675 is well tolerated and the number of angiogenic islets in the pancreas of SAR131675-treated mice is significantly decreased by 42%, compared with the vehicle-treated group. In the intervention study, daily oral administration of SAR131675 from week 10 to week 12.5 causes a significant decrease in tumor burden by 62%. Treatment with SAR131675 significantly reduces the tumor volume 24% and 50% at 30 mg/kg/d and 100 mg/kg/d, respectively. |
|In vitro||DMSO||30 mg/mL (83.7 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.