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Epothilone B/埃博霉素B {[allProObj[0].p_purity_real_show]}

货号:A301383 同义名: 帕妥匹隆 / EPO 906; Patupilone

Epothilone B是一种微管稳定剂,可以促进微管蛋白的聚合。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Epothilone B/埃博霉素B 化学结构 CAS号:152044-54-7
Epothilone B/埃博霉素B 化学结构
CAS号:152044-54-7
Epothilone B/埃博霉素B 3D分子结构
CAS号:152044-54-7
Epothilone B/埃博霉素B 化学结构 CAS号:152044-54-7
Epothilone B/埃博霉素B 3D分子结构 CAS号:152044-54-7
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Epothilone B/埃博霉素B 纯度/质量文件 产品仅供科研

货号:A301383 标准纯度: {[allProObj[0].p_purity_real_show]}
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Epothilone B/埃博霉素B 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].
体内研究

Partial tumor growth suppression occurs with either Epothilone B (Patupilone) or ionizing radiation treatment alone over ten days. However, their combined application significantly enhances tumor growth control, resulting in complete tumor regression during the follow-up period (P<0.005 for either treatment alone versus combined treatment)[3].

体外研究

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].

Epothilone B/埃博霉素B 细胞实验

Cell Line
Concentration Treated Time Description References
SKOV-3 cells 10 µM 12 hours Evaluate ROS responsiveness and drug release of Z-E ADCN in SKOV-3 cells J Nanobiotechnology. 2024 Aug 21;22(1):502.
SN neurons 5 nM 12 hours To simulate ICH and investigate the effect of EpoB on microtubule stabilization J Am Heart Assoc. 2018 Jan 18;7(2):e007626.
HeLa 67 nM 72 hours Measure cytotoxicity, IC50 value was 67 nmol/L Int J Mol Sci. 2017 Jul 9;18(7):1472.
A549 163 nM 72 hours Measure cytotoxicity, IC50 value was 163 nmol/L Int J Mol Sci. 2017 Jul 9;18(7):1472.
ES-2-luc cells 0.4 nM 2 weeks Evaluate the clonogenic inhibition effect of Epothilone B on ES-2-luc cells, showing a 25% inhibition rate. J Control Release. 2017 Dec 28;268:176-183.
HCT15 cells 50 µg/ml 24 hours To compare the apoptosis-inducing effects of UTD1 and paclitaxel in ABCB1 high-expression cells, UTD1 showed stronger apoptosis-inducing ability Cell Death Dis. 2021 Apr 1;12(4):338.
NR8383 cells 1 nM or 5 nM 3 or 5 days To evaluate the effect of Epothilone B on the proliferation of NR8383 cells. Results showed that Epothilone B inhibited the division of NR8383 cells. Cell Death Dis. 2017 Nov 2;8(11):e3162.
Human ovarian carcinoma cell line 1A9/B10 5 nM 4 days Evaluate the cytotoxicity of Epothilone B on 1A9/B10 cells Proc Natl Acad Sci U S A. 2000 Mar 14;97(6):2904-9.
Human ovarian carcinoma cell line 1A9/A8 5 nM 4 days Evaluate the cytotoxicity of Epothilone B on 1A9/A8 cells Proc Natl Acad Sci U S A. 2000 Mar 14;97(6):2904-9.
Human ovarian carcinoma cell line 1A9 0.5 nM 4 days Evaluate the cytotoxicity of Epothilone B on 1A9 cells Proc Natl Acad Sci U S A. 2000 Mar 14;97(6):2904-9.
Human ovarian carcinoma cell line 1A9 0.5 nM 4 days To select Epothilone B-resistant sublines Proc Natl Acad Sci U S A. 2000 Mar 14;97(6):2904-9.
Epothilone B-resistant subline 1A9/A8 5 nM 5 hours To evaluate tubulin polymerization in resistant cells Proc Natl Acad Sci U S A. 2000 Mar 14;97(6):2904-9.
DAOY 0.19 nM (IC50) 72 hours To evaluate the antiproliferative and cytotoxic effects of Epothilone B on DAOY cells, showing an IC50 of 0.19 nM Neuro Oncol. 2011 Sep;13(9):1000-10.
D425Med 0.37 nM (IC50) 72 hours To evaluate the antiproliferative and cytotoxic effects of Epothilone B on D425Med cells, showing an IC50 of 0.37 nM Neuro Oncol. 2011 Sep;13(9):1000-10.
D341Med 0.53 nM (IC50) 72 hours To evaluate the antiproliferative and cytotoxic effects of Epothilone B on D341Med cells, showing an IC50 of 0.53 nM Neuro Oncol. 2011 Sep;13(9):1000-10.
MEF3.8 cells 9.3 nM (IC50) 72 hours To evaluate the sensitivity of MEF3.8 cells to Epothilone B, results showed that MRP7-transfected cells exhibited 3.3-fold resistance to Epothilone B. Cancer Res. 2009 Jan 1;69(1):178-84.
HEK293 cells 0.99 nM (IC50) 72 hours To evaluate the sensitivity of HEK293 cells to Epothilone B, results showed that MRP7-transfected cells exhibited 5.3-6.8-fold resistance to Epothilone B. Cancer Res. 2009 Jan 1;69(1):178-84.
ES-2-luc cells 0.427 nM (IC50) 72 hours Evaluate the antiproliferative effect of Epothilone B on ES-2-luc cells, showing an IC50 value of 0.427 nM, which is more potent than paclitaxel. J Control Release. 2017 Dec 28;268:176-183.
HCT116 cells 0.77 µg/ml (IC50) 72 hours To evaluate the direct effect of UTD1 on CRC cell proliferation, results showed UTD1 significantly inhibited proliferation of RKO and HCT116 cells Cell Death Dis. 2021 Apr 1;12(4):338.
RKO cells 0.38 µg/ml (IC50) 72 hours To evaluate the direct effect of UTD1 on CRC cell proliferation, results showed UTD1 significantly inhibited proliferation of RKO and HCT116 cells Cell Death Dis. 2021 Apr 1;12(4):338.
MDA-MB-231 breast cancer cells 10 nM 72 hours To evaluate the cytotoxic effect of Epothilone B on MDA-MB-231 cells, showing significant reduction in cell proliferation. The Effect of Delivery System and Polymer Composition on Drug Release and Cytotoxicity against MDA-MB-231 Breast Cancer Cells. Pharmaceutics.
MIAPaCa-2 cells 0 nM, 0.1 nM, 0.2 nM, 0.4 nM, 0.8 nM Validate the inhibitory effect of Epothilone B on pancreatic cancer cell line MIAPaCa-2 J Immunother Cancer. 2023 Sep;11(9):e007466.

Epothilone B/埃博霉素B 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats Thoracic spinal cord dorsal hemisection Intraperitoneal injection 0.75 mg/kg Administered at day 1 and 15 post-injury Reduced fibrotic scar tissue, promoted axon regeneration and improved motor function recovery Systemic administration of epothilone B promotes axon regeneration after spinal cord injury. Science
Sprague-Dawley rats Spinal cord injury model Intraperitoneal injection 0.75 mg/kg Once at 1 day and once at 15 days post-injury Epothilone B reduced scar formation after spinal cord injury, promoted axonal regeneration, and improved motor function. Neural Regen Res. 2017 Mar;12(3):478-485
C57/BL6 mice ICH model Intraperitoneal injection 1.5 mg/kg Administered 2 hours after ICH surgery EpoB alleviated nigrostriatal pathway injury and improved motor function associated with microtubule stabilization by increasing the expression of acetylated a-tubulin J Am Heart Assoc. 2018 Jan 18;7(2):e007626.
Nude mice D425Med xenograft model Intravenous injection 2 mg/kg Single dose To evaluate the efficacy of combined treatment with Epothilone B and ionizing radiation on D425Med xenografts, showing complete tumor regression Neuro Oncol. 2011 Sep;13(9):1000-10.
Athymic nude mice ES-2-luc ovarian cancer xenograft model Intraperitoneal injection 2.0 mg/kg (Epothilone B), 15.0 mg/kg (17-AAG), 7.5 mg/kg (rapamycin) Single injection Evaluate the antitumor efficacy of Epothilone B combined with 17-AAG and rapamycin in an ES-2-luc ovarian cancer xenograft model, showing that a single intraperitoneal injection of g-EAR significantly delayed tumor growth with a median survival time of 58 days. J Control Release. 2017 Dec 28;268:176-183.
Nude mice RKO cell xenograft model Intraperitoneal injection 2.5 mg/kg and 5 mg/kg Every two days for 20 days To evaluate the antitumor activity of UTD1 in vivo, results showed UTD1 significantly inhibited tumor growth and was more effective and safer than paclitaxel and 5-FU Cell Death Dis. 2021 Apr 1;12(4):338.
Sprague-Dawley rats Spinal cord injury model Intraperitoneal injection 2x0.75 mg/kg Single injection To evaluate the effect of Epothilone B on functional recovery after spinal cord injury. Results showed that Epothilone B reshaped the SCI microenvironment by increasing cytokine secretion, which inhibited functional recovery. Cell Death Dis. 2017 Nov 2;8(11):e3162.
Nude mice SKOV-3 tumor model Intravenous injection 5 mg/kg and 10 mg/kg Every 3 days for 24 days Evaluate antitumor efficacy of Z-E ADCN in SKOV-3 tumor model J Nanobiotechnology. 2024 Aug 21;22(1):502.

Epothilone B/埃博霉素B 动物研究

Dose Mice: 2.5 mg/kg - 5 mg/kg[3] (i.v.); 0.75 mg/kg - 1.5 mg/kg[4] (i.p.) Rat: 0.75 mg/kg[5] (i.p.)
Administration i.v., i.p.

Epothilone B/埃博霉素B 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 - -

Epothilone B/埃博霉素B 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.

Epothilone B/埃博霉素B 实验方案

计算器
存储液制备 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

Epothilone B/埃博霉素B 技术信息

CAS号152044-54-7
分子式C27H41NO6S
分子量 507.68
SMILES Code O=C(C[C@H](O)C1(C)C)O[C@H](/C(C)=C/C2=CSC(C)=N2)C[C@]3([H])O[C@]3(C)CCC[C@H](C)[C@H](O)[C@@H](C)C1=O
MDL No. MFCD02101921
别名 帕妥匹隆 ;EPO 906; Patupilone; (-)-Epothilone B; EPO 906A; Epo B
运输蓝冰
InChI Key QXRSDHAAWVKZLJ-PVYNADRNSA-N
Pubchem ID 448013
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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