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SAR131675
| Product Name | SAR131675 |
| Price: | Inquiry |
| Catalog No.: | CN00270 |
| CAS No.: | 1433953-83-3 |
| Molecular Formula: | C18H22N4O4 |
| Molecular Weight: | 358.39 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | COC[C@@](C#Cc1ccc2c(n1)n(CC)c(c(c2=O)C(=O)NC)N)(O)C |
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| Description | SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM. |
| Target | VEGFR3:23 nM (IC50) |
| In Vitro | AR131675 is highly selective for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. However, it is moderately active on VEGFR-2 with a VEGFR-3/VEGFR-2 ratio of about 10. SAR131675 inhibits VEGFR-3 tyrosine kinase activity and VEGFR-3 autophosphorylation in HEK cells with IC50 values of 20 and 45 nM, respectively. 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. SSAR131675 has no antiproliferative activity on a panel of 30 tumors and primary cells, further showing its high specificity and indicating that SAR131675 is not a cytotoxic or cytostatic agent[1]. |
| In Vivo | SAR131675 is very well tolerated in mice and shows a potent antitumoral effect in several orthotopic and syngenic models, including mammary 4T1 carcinoma and RIP1.Tag2 tumors. Interestingly, it significantly reduces lymph node invasion and lung metastasis, showing its antilymphangiogenic activity in vivo. SAR131675 significantly reduces TAM infiltration and aggregation in 4T1 tumors[1]. |
| Cell Assay | HLMVECs are seeded in 96-well plates coated with 0.3% gelatin (5000 cells per well). Cells are incubated in RPMI 0.1% FCS with VEGFA (10 ng/mL) VEGFC (300 ng/mL), VEGFD (300 ng/mL), or FGF2 (10 ng/mL) in the absence or presence of SAR131675. Five days later, viable cells are quantified with the cell Titer-glo luminescent cell viability assay[1]. |
| Animal Admin | Mouse: Sterile sponge disks impregnated with 200 μg of FGF2 or PBS are subcutaneously introduced on the back of anaesthetized mice. FGF2 is reinjected into the sponges the first 2 days. Daily oral treatment with SAR131675 (30, 100, and 300 mg/kg/d) started the day of sponge implantation. Seven days later, the animals are euthanatized and the sponges are removed, harvested, and lysed in RIPA buffer at 4°C. After a centrifugation at 6,000 × g, the supernatants are collected for further analysis[1]. |
| Density | 1.3±0.1 g/cm3 |
| Boiling Point | 592.2±50.0 °C at 760 mmHg |
| Flash Point | 312.0±30.1 °C |
| Exact Mass | 358.164093 |
| PSA | 119.47000 |
| LogP | -0.61 |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Storage condition | -20℃ |