PDGFR/Flk-1/FGFR1 inhibitor,potent and competitive
Sample solution is provided at 25 µL, 10mM.
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|Description||TSU-68 (SU6668, Orantinib) is a potent inhibitor of PDGFR with a Ki value of 8 nM.|
|IC50||8 nM (Ki)||1.2 μM(Ki)||2.1 μM(Ki)|
|Cas No.||252916-29-3||SDF||Download SDF|
|Chemical Name||3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid|
|Solubility||>15.5mg/mL in DMSO||Storage||Store at -20°C|
Ki: Flk-1trans-phosphorylation (2.1 mM), FGFR1 trans-phosphorylation (1.2 mM), and PDGFR autophosphorylation (0.008 mM).
Vascular endothelial growth factor, fibroblast growth factor (FGF), and platelet-derived growth factor (PDGF) and their cognate receptor tyrosine kinases are strongly implicated in angiogenesis associated with solid tumors. TSU-68 is a novel inhibitor of these receptors.
In vitro: Biochemical kinetic studies using isolated Flk-1, FGF receptor 1, and PDGF receptor β kinases revealed that TSU-68 has competitive inhibitory properties with respect to ATP. In cellular systems, TSU-68 inhibited receptor tyrosine phosphorylation and mitogenesis after stimulation of cells by appropriate ligands .
In vivo: Oral or i.p. administration of TSU-68 in athymic mice resulted in significant growth inhibition of a diverse panel of human tumor xenografts of glioma, melanoma, lung, colon, ovarian, and epidermoid origin .
Clinical trial: Phase I clinical study indicated that TSU-68 can be safely combined with standard doses of carboplatin-paclitaxel, with the combination manifesting promising antitumor activity .
 Laird AD, Vajkoczy P, Shawver LK et al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60.
 Okamoto I, Yoshioka H, Takeda K et al. Phase I clinical study of the angiogenesis inhibitor TSU-68 combined with carboplatin and paclitaxel in chemotherapy-naive patients with advanced non-small cell lung cancer. J Thorac Oncol. 2012 Feb;7(2):427-33.