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SAR131675

Cat. No. M2078
SAR131675 Structure
Synonym:

CAS#: 1092539-44-0

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50mg USD 220 In stock
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Quality Control
Biological Activity

SAR131675 is the first highly specific VEGFR-3-TK inhibitor, which displaying significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion. SAR131675 inhibited VEGFR-3 tyrosine kinase activity and VEGFR-3 autophosphorylation in HEK cells with IC50 values of 20 and 45 nmol/L, respectively. SAR131675 dose dependently inhibited the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC50 of about 20 nmol/L. SAR131675 showed a potent antitumoral effect in several orthotopic and syngenic models, including mammary 4T1 carcinoma and RIP1.Tag2 tumors. Interestingly, SAR131675 significantly reduced lymph node invasion and lung metastasis, showing its antilymphangiogenic activity in vivo. SAR131675 significantly reduced TAM infiltration and aggregation in 4T1 tumors.

Customer Product Validations & Biological Datas
Source Mol Cancer Ther (2012). Figure 2. SAR131675
Method migration assay
Cell Lines lymphatic cells
Concentrations 30–300 nmol/L
Incubation Time 5 d
Results SAR131675 potently inhibited VEGFCinduced migration with an IC50 < 30 nmol/L (Fig. 2B) and VEGFA-induced migration with an IC50 of about 100 nmol/L
Source Mol Cancer Ther (2012). Figure 1. SAR131675
Method migration assays
Cell Lines HEK cells
Concentrations 100 mmol/L
Incubation Time 1 h
Results SAR131675 was seen to be cell permeable and inhibited VEGFR-3 autophosphorylation in a dose dependent manner with an IC50 ranging from 30 to 50 nmol/L
Protocol
Cell Experiment
Cell lines HEK cell
Preparation method Experiments were conducted as described previously (35). Twenty-four hours after transfection, the cells were treated during 1 hour with orthovanadate (100 mmol/L), harvested, collected, and, after counting, distributed in 5-mL tubes in the presence of the indicated concentration of SAR131675.
Concentrations 3–1,000 nmol/L
Incubation time 30 min
Animal Experiment
Animal models Tag2/transgenic mouse
Formulation 0.6% methylcellulose/0.5% Tween 80 solution
Dosages 30, 100, and 300 mg/kg/d
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 358.39
Formula C18H22N4O4
CAS Number 1433953-83-3
Purity >99%
Solubility DMSO: ≥ 25 mg/mL
Storage at -20°C
References

Specific Inhibition of the VEGFR-3 Tyrosine Kinase by SAR131675 Reduces Peripheral and Tumor Associated Immunosuppressive Myeloid Cells.
Espagnolle N, et al. Cancers (Basel). 2014 Feb 28;6(1):472-90. PMID: 24589997.

SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities.
Alam A, et al. Mol Cancer Ther. 2012 Aug;11(8):1637-49. PMID: 22584122.

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Abmole Inhibitor Catalog 2017




Keywords: SAR131675, CAS#: 1092539-44-0 supplier, VEGFR/PDGFR, inhibitors

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