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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.
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SAR131675 purchased from AbMole
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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 |
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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 |
| 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 |
| Molecular Weight | 358.39 |
| Formula | C18H22N4O4 |
| CAS Number | 1433953-83-3 |
| Solubility (25°C) | DMSO ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related VEGFR/PDGFR Products |
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| Conbercept
Conbercept (KH902) is a monoclonal antibody targeting VEGFRA fused to the IGHG1 Fc fragment. Conbercept is produced by the fusion of the second C-LIKE of FLT1 and the third and fourth C-LIKE of KDR with IGHG1 Fc. |
| SU5208
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2). |
| VEGFR-IN-1
VEGFR-IN-1 is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively. |
| (Z)-Orantinib
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. |
| (Rac)-SAR131675
(Rac)-SAR131675 is the racemate of SAR131675. |
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