生物活性 | |||
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描述 | Epothilone B is a microtubule stabilizer with a Ki of 0.71μM, which acts by binding to the αβ-tubulin heterodimer subunit which causes decreasing of αβ-tubulin dissociation[1]. Epothilone B displays potent cytotoxic activity against HCT116 cells, with an IC50 value of 0.8 nM in a cytotoxicity assay[1]. As a microtubule-targeting compound, Epothilone B (Patupilone) effectively hinders cell proliferation, evidenced by an IC50 of 6 nM in MTT cell proliferation assays after 72 hours of treatment. Concentrations of Epothilone B ≤1 nM do not exhibit cytotoxic effects. At a non-toxic concentration of 1 nM, Epothilone B significantly curtails transwell cell migration, with an increased effect observed at 10 nM[2]. In human medulloblastoma cell lines, Epothilone B (Patupilone) acts as a novel, non-taxane microtubule stabilizer without neurotoxic effects. It diminishes proliferative activity in D341, D425Med, and DAOY cell lines with IC50 values of 0.53 nM, 0.37 nM, and 0.19 nM, respectively. The impact on clonogenic survival in the D341Med cell line mirrors the effects on proliferative activity (IC50, 0.50-0.75 nM), whereas D425Med and DAOY cell clonogenicity significantly drops at ten times lower Epothilone B concentrations (IC50, 30 pM), showcasing its high efficacy against various medulloblastoma cell lines[3]. |
细胞研究 | |||||
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细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
human 639-V cell | Growth inhibition assay | Inhibition of human 639-V cell growth in a cell viability assay, IC50=0.218 μM | SANGER | ||
human 786-0 cell | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50=0.11 nM | SANGER | ||
human A375 cell | Growth inhibition assay | Inhibition of human A375 cell growth in a cell viability assay, IC50=5e-05 μM | SANGER |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00077259 | Colorectal Cancer | Phase 2 | Completed | - | United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 收起 << |
NCT00080301 | Breast Cancer ... 展开 >> Metastases 收起 << | Phase 3 | Completed | - | - |
NCT00080301 | - | Completed | - | - |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.97mL 0.39mL 0.20mL |
9.85mL 1.97mL 0.98mL |
19.70mL 3.94mL 1.97mL |
参考文献 |
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