| 备注 |
SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc. |
| 生化机理 |
VEGFR-3 is a tyrosine kinase receptor recognized by VEGF-C and VEGF-D and plays a major role in lymphangiogenesis. A number of clinical and experimental studies have demonstrated that tumor lymphangiogenesis induced by VEGFR-3 promotes metastasis to regional lymph nodes. SAR131675 is a potent and selective VEGFR-3 inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities. SAR131675 inhibited VEGFR-3 tyrosine kinase activity and VEGFR-3 autophosphorylation in HEK cells with IC(50) values of 20 and 45 nmol/L, respectively. |
| 别名 |
(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;(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 |
