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SAR131675 is an ATP-competitive inhibitor of VEGF receptor 3 (VEGFR3) with an IC50 value of 23 nM for the human recombinant receptor in a cell-free assay.{46458} It is selective for VEGFR3 over VEGFR2 and VEGFR1 (IC50s = 230 and >3,000 nM, respectively). SAR131675 inhibits survival of human lymphatic cells cultured with the VEGFR3-specific ligands VEGF-C and VEGF-D over the non-specific ligand VEGF-A in vitro (IC50s = 14, 17, and 664 nM, respectively). It decreases VEGF-C and VEGF-A-induced migration of human microvascular endothelial cells (HMVECs) when used at concentrations of 100 and 300 nM. SAR131675 (100 mg/kg) reduces tumor size, decreases the number of pancreatic angiogenic islets, and increases survival in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors. It also decreases tumor size, levels of VEGFR3 in mammary tumor lysates, number of tumor-associated macrophages in mammary tumors, and the number of lung metastases in a 4T1 mouse allograft model when administered at a dose of 100 mg/kg.
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 25 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1433953-83-3 |
| Molecular formula | C18H22N4O4 |
| Smiles | COC[C@@](O)(C)C#CC1=NC(N(CC)C(N)=C(C(NC)=O)C2=O)=C2C=C1 |
| Molecular weight | 358,4 |
| Custom code | 2921.29 |
| Formulation | A crystalline solid |
| Purity | ≥98% |
| UNSPSC code | 12352100 |
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.
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