Antibodies
Epothilone A
- 貨號 Cat. No.
- S1297
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
Epothilone A
Catalog No.S1297
Epothilone A is a Taxol-like microtubule-stabilizing agent with EC0.01 of 2 μM.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Epothilone A is a Taxol-like microtubule-stabilizing agent with EC0.01 of 2 μM. | |||||
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| Targets | Tubulin | |||||
| IC50 | 2 μM (EC0.01) [1] | |||||
| In vitro | Epothilone A, discovered from the myxobacterium Sorangium cellulosum, is a Taxol-like microtubule-stabilizing agent that induces tubulin polymerization, leading to cell cycle arrest at the G2-M transition, cytotoxicity, and apoptosis. Epothilone A potently inhibits cell proliferation in HCT116 cells, with IC50 of 4.4 nM. [1] Epothilone A also displays cytotoxicity in KB3-1, KBV-1, Hela, and Hs578T cells, with IC50 values ranging from 13 nM to 160 nM. Epothilone A is more water soluble than Taxol and competes with Taxol in binding with microtubules, with IC50 of 2.3 μM. [2] However, both Epothilone A and Taxol don’t share a common pharmacophore and exploits the tubulin-binding pocket uniquely and independently. [3] Recently, it is found that microbiological transformation of Epothilone A by Aspergillus niger AS 3.739 yields several metabolites that is also toxic to MCF-7 cells, but with much higher IC50 values. [4] | |||||
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Protocol(Only for Reference)
Kinase Assay: [1]
| Tubulin polymerization assay | Calf brain microtubule proteins (MTP) are purified, which includes approximately 15%–20% microtubule associated proteins. The buffer (MES buffer) used for the Epothilone A-microtubule studies contains 0.1 M 2-morpholinoethanesulfonic acid (MES), 1 mM EGTA, 0.5 mM MgCl2, and 3 M glycerol at pH 6.6. Samples for electron microscopy are placed on carbon-over-Parlodion-coated grids (300 mesh) and negatively stained with 2% uranyl acetate. Microtubule assembly in the presence or absence of Epothilone A is monitored spectrophotometrically by using a spectrophotometer equipped with a thermostatically regulated liquid circulator. The temperature is held at 35 °C and changes in turbidity (representative of polymer mass) are monitored at 350 nm. Effective concentration (EC0.01), defined as the interpolated concentration capable of inducing an initial slope of 0.01 OD/min rate, is calculated using the formula EC0.01 = concentration/slope and expressed as the mean with standard deviation obtained from three different concentrations. |
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Cell Assay: [2]
| Cell lines | KB3-1, KBV-1, Hela, and Hs578T cells |
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| Concentrations | 0–2 μM |
| Incubation Time | 24 hours for mitotic arrest or 72 hours for cytotoxicity |
| Method | For mitotic block and aberrant mitosis, cells are plated either in 48-well plates (for trypan blue and cell counting) or onto coverslips. After 24 hours, cells are treated with Epothilone A and are scored at regular intervals. For the cytotoxicity analysis, cells are counted and scored as trypan blue positive or negative. Concurrently, coverslips and aliquots of cells in the culture supernatant are fixed and stained with Hoechst 33342 in PBS. These cells are scored for cells blocked at the G2-M transition and aberrant mitosis. |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01454479 | Enrolling by invitation | Recurrent Endometrial Cancer | Chang Gung Memorial Hospital|Hung-Hsueh Chou|GlaxoSmithKline|Bristol-Myers Squibb | 2011-03 | Phase 1 |
| NCT01375829 | Recruiting | Unspecified Adult Solid Tumor, Protocol Specific | National Cancer Institute (NCI) | 2011-06 | Phase 1 |
| NCT01379287 | Recruiting | Solid Tumors | Memorial Sloan-Kettering Cancer Center|University of Pittsburgh|Bristol-Myers Squibb | 2011-06 | Phase 1 |
| NCT01818999 | Not yet recruiting | METASTATIC BREAST CANCER | University of Texas Southwestern Medical Center | 2013-04 | Phase 2 |
| NCT01349088 | Not yet recruiting | Breast Cancer|Metastatic Breast Cancer|Stage IV Breast Cancer | Thomas Jefferson University|Susan G. Komen Breast Cancer Foundation|Amgen | 2013-12 | Phase 1|Phase 2 |
Chemical Information
| Molecular Weight (MW) | 493.66 |
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| Formula | C26H39NO6S |
| CAS No. | 152044-53-6 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 99 mg/mL (200 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 99 mg/mL (200 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | (1S,3S,7S,10R,11S,12S,16R,E)-7,11-dihydroxy-8,8,10,12-tetramethyl-3-(1-(2-methylthiazol-4-yl)prop-1-en-2-yl)-4,17-dioxa-bicyclo[14.1.0]heptadecane-5,9-dione |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.49366 | 4.9366 | 9.8732 | 14.8098 |
