SAR131675

Catalog No.S2842

SAR131675 Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 270 In stock

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2 Customer Reviews

  • 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.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

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.
Targets
VEGFR3 [1]
(Cell-free assay)
23 nM
In vitro

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. [1]

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. [1]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: BALB/c mice with 4T1 cells
  • Formulation: Dissolved on the day of use in a 0.6% methylcellulose/0.5% Tween 80 solution.
  • Dosages: 30 mg/kg/d, 100 mg/kg/d, and 300 mg/kg/d
  • Administration: Oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 30 mg/mL (83.7 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 0.5% CMC+0.25% Tween 80 20 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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.

Chemical Information

Molecular Weight 358.39
Formula

C18H22N4O4

CAS No. 1433953-83-3
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID