Epothilone A/埃博霉素 A
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货号：A408460同义名：
西洛他唑A
/ Epo A
Epothilone A是一种类似紫杉醇的微管稳定剂，EC0.01 值为 2 μM。
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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
Epothilone A competitively inhibits the binding of [3H] paclitaxel to tubulin polymers. The apparent Ki value for Epothilone A is 1.4 μM according to Hanes analysis and 0.6 μM according to Dixon analysis[1]. Epothilone A demonstrates high cytotoxicity (IC50=0.05 μM) in vitro against the human T-24 bladder carcinoma cell line. In competition assays, the binding affinity of Epothilone A to tubulin is comparable to that of paclitaxel. The IC50 values for displacing 100 nM of (3H) paclitaxel from the tubulin binding site are 3.6 μM for paclitaxel, 2.3 μM for Epothilone A, and 3.3 μM for patupilone[2].
体外研究
Epothilone A competitively inhibits the binding of [3H] paclitaxel to tubulin polymers. The apparent Ki value for Epothilone A is 1.4 μM according to Hanes analysis and 0.6 μM according to Dixon analysis[1].
Epothilone A demonstrates high cytotoxicity (IC50=0.05 μM) in vitro against the human T-24 bladder carcinoma cell line. In competition assays, the binding affinity of Epothilone A to tubulin is comparable to that of paclitaxel. The IC50 values for displacing 100 nM of (3H) paclitaxel from the tubulin binding site are 3.6 μM for paclitaxel, 2.3 μM for Epothilone A, and 3.3 μM for patupilone[2].
Epothilone A/埃博霉素 A 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Multidrug resistant cancer cell line NCI/ADR-RES
140 ± 20 nM
Evaluation of cytotoxicity of Epothilone A against NCI/ADR-RES cells, IC50 value of 140 ± 20 nM.
J Med Chem. 2016 Apr 14;59(7):3499-514.
Human ovarian cancer cell line OVCAR-8
7.0 ± 1 nM
Evaluation of cytotoxicity of Epothilone A against OVCAR-8 cells, IC50 value of 7.0 ± 1 nM.
J Med Chem. 2016 Apr 14;59(7):3499-514.
CHO cells
0-10 nM
7 days
To evaluate the antiproliferative effect of Epothilone A on CHO cells, results showed that cells overexpressing MCAK had 2-3 fold resistance to Epothilone A.
Mol Cancer Ther. 2011 Jun;10(6):929-37.
A2780-Epo B human ovarian cancer cells
3 nM
18 hours
No effect on p53 nuclear accumulation
Proc Natl Acad Sci U S A. 2002 Aug 6;99(16):10855-60.
A2780 human ovarian cancer cells
3 nM
18 hours
Enhanced p53 nuclear accumulation and induced mdm2
Proc Natl Acad Sci U S A. 2002 Aug 6;99(16):10855-60.
A549 human lung cancer cells
3 nM
18 hours
Enhanced p53 nuclear accumulation and induced mdm2
Proc Natl Acad Sci U S A. 2002 Aug 6;99(16):10855-60.
EpoA-resistant subline 1A9/A8
150 nM to 5000 nM
5 hours
Evaluation of microtubule polymerization in resistant cells, showing impaired polymerization even at high EpoA concentrations
Proc Natl Acad Sci U S A. 2000 Mar 14;97(6):2904-9.
Human ovarian carcinoma cell line A2780 (1A9)
6 nM
Selection of resistant sublines, yielding EpoA-resistant subline 1A9/A8
Proc Natl Acad Sci U S A. 2000 Mar 14;97(6):2904-9.
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