| CAS NO: | 252916-29-3 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 252916-29-3 |
| 别名 | SU6668; TSU-68 |
| 化学名 | 3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid |
| Canonical SMILES | CC1=C(NC(=C1CCC(=O)O)C)C=C2C3=CC=CC=C3NC2=O |
| 分子式 | C18H18N2O3 |
| 分子量 | 310.35 |
| 溶解度 | ≥ 15.5mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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 [1]. 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 [1]. 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 [2]. References: |
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