Epothilone B

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Chemical Structure| 152044-54-7 同义名 : 帕妥匹隆 ;EPO 906;Patupilone;(-)-Epothilone B;EPO 906A;Epo B
CAS号 : 152044-54-7
货号 : A301383
分子式 : C27H41NO6S
纯度 : 99%+
分子量 : 507.683
MDL号 : MFCD02101921
存储条件:

Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(206.82 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
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
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
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
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

[1]Regueiro-Ren A, et al. Synthesis and biological activity of novel epothilone aziridines. Org Lett. 2001 Aug 23;3(17):2693-6.

[2]Pagano A, et al. Epothilone B inhibits migration of glioblastoma cells by inducing microtubule catastrophes and affecting EB1 accumulation at microtubule plus ends. Biochem Pharmacol. 2012 Aug 15;84(4):432-43.

[3]Oehler C, et al. The microtubule stabilizer patupilone (epothilone B) is a potent radiosensitizer in medulloblastoma cells. Neuro Oncol. 2011 Sep;13(9):1000-10.