An ATP-competitive inhibitor of VEGFR3 (IC50 = 23 nM); selective for VEGFR3 over VEGFR2 and VEGFR1 (IC50s = 230 and >3

SAR131675 – 1 mg

Brand:
Cayman
CAS:
1433953-83-3
Storage:
-20
UN-No:
Non-Hazardous - /

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.  

 

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Description

An ATP-competitive inhibitor of VEGFR3 (IC50 = 23 nM); selective for VEGFR3 over VEGFR2 and VEGFR1 (IC50s = 230 and >3,000 nM, respectively); inhibits survival of human lymphatic cells cultured with the VEGFR3 ligands VEGF-C and VEGF-D over the non-specific ligand VEGF-A in vitro (IC50s = 14, 17, and 664 nM, respectively); decreases VEGF-C and VEGF-A-induced migration of HMVECs at 100 and 300 nM; reduces tumor size, decreases the number of pancreatic angiogenic islets, and increases survival in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors at 100 mg/kg; 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 at 100 mg/kg

Formal name: 2-amino-1-ethyl-1,4-dihydro-7-[(3R)-3-hydroxy-4-methoxy-3-methyl-1-butyn-1-yl]-N-methyl-4-oxo-1,8-naphthyridine-3-carboxamide

Synonyms: 

Molecular weight: 358.4

CAS: 1433953-83-3

Purity: ≥98%

Formulation: A crystalline solid

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