货号 | 5109/50 |
别名 | N-(3-Aminopropyl)-N-[(1R)-1-[7-chlo |
供应商 | Tocris |
生物活性 | Potent kinesin spindle protein (KSP) inhibitor (Ki = 0.1 nM). Induces cell mitotic arrest and apoptosis in vitro. Inhibits the growth of a range of tumor cells in vitro, including colon (HCT 116), prostate (PC-3) and leukemia (K-562) cancer cell lines. Causes tumor regression in human tumor xenograft models in vivo, including colon (Colo205), lung (H69) and breast (MCF7) cancer cell xenografts. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 553.52 |
分子式 | C31H33ClN2O3 |
可溶性/溶解性 | Soluble to 100 mM in DMSO |
参考文献 | Goodet al (2013) Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models. J.Med.Chem. 56 1878. PMID: 23394180. Talapatraet al (2013) Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism. J.Med.Chem. 56 6317. PMID: 23875972. Jacksonet al (2006) A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer. First AACR International Conference on Molecular and Diagnostics in Cancer Therapeutic Development. Abstract (B11). |