SAR131675 MedChemExpress (MCE)

Product Name	SAR131675
Synonyms	CS-994 SAR131675 SAR 131675 (R)-2-amino-1-ethyl-7-(3-hydroxy-4-methoxy-3-methylbut-1-ynyl)-N-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide 1,8-Naphthyridine-3-carboxamide, 2-amino-1-ethyl-1,4-dihydro-7-[(3R)-3-hydroxy-4-methoxy-3-methyl-1-butyn-1-yl]-N-methyl-4-oxo-
CAS	1433953-83-3
EINECS
Chemical Formula	C18H22N4O4
Molecular Weight	358.39
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	SAR131675 SAR131675 MedChemExpress (MCE) HY-15458 1433953-83-3 99.76% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions SAR131675 SAR131675 MedChemExpress (MCE) HY-15458 1433953-83-3 99.76% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM. SAR131675 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. AR131675 is highly selective for VEGFR-3. 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]. 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]. Despite the promising findings, SAR131675 development was terminated during preclinical development due to adverse metabolic effects[2]. 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]. 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]. Multiwell plates are precoated with a synthetic polymer substrate poly-Glu-Tyr (polyGT 4:1). The reaction is carried out in the presence of kinase buffer (10×: 50 mM HEPES buffer, pH 7.4, 20 mM MgCl2, 0.1 mM MnCl2, and 0.2 mM Na3VO4) supplemented with ATP and dimethyl sulfoxide (DMSO) for the positive control (C+) or SAR131675 (ranging from 3-1,000 nM). ATP is used at 30 μM for VEGFR-1 and VEGFR-3 and at 15 μM for VEGFR-2. The phosphorylated poly-GT is probed with a phosphotyrosine specific monoclonal antibody (mAb) conjugated to horseradish peroxidase and developed in the dark with the HRP chromogenic substrate (OPD). The reaction is then stopped by the addition of 100 μL 1.25 mol/L H2SO4, and absorbance is determined using an Envision spectrophotometer at 492 nm[1]. VEGFR3 23 nM (IC50) \| \| \| \| \| \| \| \| \| \| [1]. Alam A, et al. SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities. Mol Cancer Ther. 2012 Aug 11(8):1637-49. [Content Brief] [2]. Paillasse MR, Esquerré M, Bertrand FA, et al. Targeting Tumor Angiogenesis with the Selective VEGFR-3 Inhibitor EVT801 in Combination with Cancer Immunotherapy. Cancer Res Commun. 2022 2(11):1504-1519. [Content Brief]
Last Update	2025-04-01 14:45:47

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