现货,Ispinesib (SB-715992),CAS号:336113-53-2,美国进口, HDAC-HSP-Aurora, Kinesin Spindle Protein , Kinesin Spindle Protein 抑制剂和化合物,selleck,目录号S1452

信号转导通路: HDAC-HSP-Aurora >> Kinesin Spindle Protein >> Kinesin Spindle Protein 抑制剂和化合物 >> Ispinesib (SB-715992)http://www.selleck.cn/ispinesib-mesilate-sb-715992-S1452.html

技术数据:

分子量(MW): 517.06

化学式:

C30H33ClN4O2

 

溶解度: DMSO ≥103mg/mL Water <1mg/mL Ethanol ≥103mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 336113-53-2

生物活性

 

 

Ispinesib (SB 715992) is a potent mitotic kinesin KSP (Eg5) inhibitor with a Ki and an IC50 of 0.6 and 4.1 nM, respectively. Ispinesib (SB 715992) has cytotoxic activity at less than 10 nM in a spectrum of tumor cell lines. Ispinesib (SB 715992) is negative in a mouse model of peripheral neuropathy in which paclitaxel is positive. Ispinesib (SB 715992) was shown to have activity against advanced human colon tumor xenografts including: Colo205 (complete regressions), Colo201 (complete regressions), and HT-29 (tumor growth delay). Ispinesib (SB 715992) (10 mg/kg) induced unexplained toxicity in mice bearing osteosarcoma xenografts. Ispinesib (SB 715992) enhanced the antitumor activity of trastuzumab, lapatinib, doxorubicin, and capecitabine and exhibited activity comparable with paclitaxel and ixabepilone. [1][2]

 

 

 

参考文献

SB-715992, a potent and selective inhibitor of KSP mitotic kinesin, demonstrates broad-spectrum activity in advanced murine tumors and human tumor xenografts Randall K. Johnson, Francis L. McCabe,et al. Pediatr Blood Cancer. 2009 Dec 15;53(7):1255-63.

Activity of the Kinesin Spindle Protein Inhibitor Ispinesib (SB-715992) in Models of Breast Cancer Jefferson Davis, Mamatha Reddy, et al. Clin Cancer Res 2010;16:566-576

 

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