N-(3-氨基丙基)-N-[(1R)-1-[7-氯-4-氧代-3-(苯基甲基)-4H-1-苯并吡喃-2-基]-2-甲基丙基]-4-甲基苯甲酰胺盐酸盐

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N-(3-氨基丙基)-N-[(1R)-1-[7-氯-4-氧代-3-(苯基甲基)-4H-1-苯并吡喃-2-基]-2-甲基丙基]-4-甲基苯甲酰胺盐酸盐

编号ABP000941 化学名称SB743921 CAS940929-33-9 分子式C31H34Cl2N2O3 分子量553.519 纯度 >99%

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化学名称 : N-(3-氨基丙基)-N-[(1R)-1-[7-氯-4-氧代-3-(苯基甲基)-4H-1-苯并吡喃-2-基]-2-甲基丙基]-4-甲基苯甲酰胺盐酸盐

CAS : 940929-33-9

英文名称: SB743921

英文同义词: (R)-N-(3-aminopropyl)-N-(1-(3-benzyl-7-chloro-4-oxo-4H-chromen-2-yl)-2-methylpropyl)-4-methylbenzamide hydrochloride

同义词: N-(3-氨基丙基)-N-[(1R)-1-[7-氯-4-氧代-3-(苯基甲基)-4H-1-苯并吡喃-2-基]-2-甲基丙基]-4-甲基苯甲酰胺盐酸盐

溶解度:DMSO

储存条件:at -20℃ 2 years

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.

参考文献

[1] Carol H et al. Pediatr Blood Cancer. 2009 Dec 15; 53(7):1255-63.