| 应用 |
An antiproliferating agent and ATP-competitive PDGFR, Flk-1/KDR (VEGF), and FGFR inhibitor |
| 产品介绍 |
TSU-68 (SU6668; Orantinib)是多酪氨酸激酶受体抑制剂，对PDGFR自磷酸化抑制性最强，Ki为8 nM，还能相对弱地抑制VEGF-R1和FGF-R1。 |
| 备注 |
SU6668 has greatest potency against PDGFR autophosphorylation with Ki of 8 nM, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit |
| 生化机理 |
TSU-68 (SU6668)is a novel multiple receptor tyrosine kinase inhibitor with IC50 of 2.1 μM, 8 nM and 1.2 μM for VEGF-R1, PDGF-Rβ and FGF-R1, respectively. |
| 别名 |
SU 6668;TSU68; 5-((1,2-二氢-2-氧代-3H-吲哚-3-亚基)甲基)-2,4-二甲基-1H-吡咯-3-丙酸;;Orantinib;TSU 68;SU6668； 5-(1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl)-2,4-dimethyl-1h-pyrrole-3-propanoic acid；3-[2,4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid; 3-[2, 4-dimethyl-5-[(E)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl] propanoic acid |
