Epothilone D
Oxacyclohexadec-13-ene-2,6-dione, 4,8-dihydroxy-5,5,7,9,13-pentamethyl-16-(1E)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl-, (4S,7R,8S,9S,13Z,16S)-
CAS: 189453-10-9
Molecular Formula: C27H41NO5S
Epothilone D - Names and Identifiers
Epothilone D - Physico-chemical Properties
| Molecular Formula | C27H41NO5S |
| Molar Mass | 491.68 |
| Density | 1.084±0.06 g/cm3(Predicted) |
| Melting Point | 63-66°C |
| Boling Point | 663.7±55.0 °C(Predicted) |
| Specific Rotation(α) | D22 -61.3° (c = 2.5 in methanol) |
| Flash Point | 355.2°C |
| Vapor Presure | 1.62E-18mmHg at 25°C |
| pKa | 13.47±0.70(Predicted) |
| Storage Condition | -20°C Freezer |
| Refractive Index | 1.522 |
| In vitro study | Epothilone D (KOS-862) is a more potent microtubule stabilizer in vitro than epothilone A or B. In vitro, Epothilone D has shown potent cytotoxicity in a panel of human tumor cell lines, with similar potency to paclitaxel. Epothilone D also shows a definite advantage over paclitaxel in drug-resistant cell lines, and retained its cytotoxicity against a multidrug resistant cell line over-expressing P-glycoprotein. Epothilone D (EpoD) is a microtubules (MTs)-stabilizing agent. |
| In vivo study | To evaluate whether Epothilone D (EpoD) improves MT and axonal function in PS19 mice, groups of 3-month old male PS19 mice received weekly i.p. injections of vehicle or Epothilone D (EpoD) (1 mg/kg or 3 mg/kg) for a total of 3 months. In addition, 3-month old non-Tg littermates received 3 mg/kg Epothilone D (EpoD) or vehicle. The 3 mg/kg Epothilone D (EpoD) dose corresponds to ~10-fold less than that used in a Phase II clinical study, which should minimize side-effects such as neutropenia that are observed with MT-stabilizing drugs in human subjects. PS19 and WT mice that receive Epothilone D (EpoD) show no signs of drug intolerance. Indeed, all drug-treated mice exhibited weight gain that is indistinguishable from vehicle-treated animals. Likewise, relative organ weights are similar in vehicle- and Epothilone D (EpoD)-treated mice. The motor performance of Epothilone D (EpoD)-treated mice, assessed using a standard rotarod test, is not significantly different from vehicle-treated cohorts. Finally, although there is minor group-to-group variability, there are no significant differences in white blood cell counts or neutrophil content between any of the treatment cohorts. Thus, the low doses of Epothilone D (EpoD) utilized in these studies appeared to be well tolerated. |
Epothilone D - Reference Information
| Overview | Epothilones are macrolide secondary metabolites produced by fibrocystic bacteria, is a new type of anti-tumor drugs. Its mechanism of action is the same as that of paclitaxel, and it inhibits the proliferation of tumor cells by promoting the polymerization of microtubules. Compared with paclitaxel, epothilone has less toxicity, better water solubility and stronger effect on paclitaxel resistant cells, it is one of the most potential new anti-tumor drugs. At present, it has significant therapeutic effect on colon cancer, breast cancer, ovarian cancer and so on. Figure 1 is the structural formula of Epothilone B |
| preparation method | biological fermentation medium: CNST medium: KNO 30.05%,Na2HPO 40.025%,MgSO4 · 7 H2O 0.1%, feC 30.001%, Agar 2%, trace element solution 1 mL/L, ph7.2. 1 * 105Pa high pressure steam sterilization 20 min. M26 Medium: potato starch 8.0g/L, soybean peptone 2.0g/L, glucose 2.0g/L, yeast powder 2.0g/L,MgSO4 · 7H2O1.0g/L, caCl21.0 g/L,EDTA-Fe3 +1 mL/L, trace elements 1 mL/L, with KOH to adjust the pH value of 7.2. Initial fermentation medium: dextrin 0.3%, sucrose 0.07%, glucose 0.02%, soybean meal 0.17%, magnesium sulfate heptahydrate 0.17%, anhydrous calcium chloride 0.3%,EDTA-Fe3 +2 mL/L, trace element (TE)0.5 mL/L,pH7.2, resin XAD-16 2%. 1 * 105Pa high pressure steam sterilization 20 min. Culture method: Seed culture: connect the strain preserved in solid slant culture medium to the CNST plate with sterilized filter paper, invert it in the constant temperature incubator at 30 ℃ for 5-7 days, transfer in M26 Medium, the volume of 50 mL/250 mL triangle bottle, at 30 ℃, 170, after 72 h of shaking culture, A seed liquid was obtained as a fermentation culture. Fermentation culture: the seed liquid was inoculated into the fermentation medium with 5%(V/V) inoculation amount for shaking culture, and the fermentation system was 300 mL triangular bottle with 50 mL liquid, under the condition of 30 C, 170 r/min, the shaking table was cultured for 5 d. |
| Application | for the treatment of colon cancer, breast cancer and ovarian cancer. The overview, preparation method and application of Epothilone B are Ding Hong editing. (2015-12-21) |
| biological activity | Epothilone D (KOS 862) is a potent microtubule stabilizer. |
| Target | microtumule/Tubulin |
| in vitro study | Epothilone D (KOS-862) is. In vitro, Epothilone D has shown potential cytotoxicity in a panel of human tumor cell lines, with similar intensity to paclitaxel. Epothilone D also show a defined advantage over paclitaxel in drug-resistant cell lines, and retained its cytotoxicity against a multidrug resistant cell line over-expressing P-glycoprotein. Epothilone D (EpoD) is a microtubules (MTs)-stabilizing agent. |
| in vivo study | To evaluate, groups of 3-month old male PS19 mice received weekly I. p. injections of vehicle or epothpiece D (EpoD) (1 mg/kg or 3 mg/kg) for a total of 3 months. In addition, 3-month old non-Tg littermates received 3 mg/kg Epothilone D (EpoD) or vehicle. The 3 mg/kg Epothilone D (EpoD) dose corresponds to ~10-fold less than that used in a Phase II clinical study which should minimize side-effects such as neutropenia that are observed with MT-stabilizing drugs in human subjects. PS19 and WT mice that receive Epothilone D (EpoD) show no signs of drug intolerance. Indeed, all drug-treated mice exhibited weight gain that is indistinguishable from vehicle-treated animals. Likewise, relative organ weights are similar in vehicle- and Epothilone D (EpoD)-treated mice. The motor performance of Epothilone D (EpoD)-treated mice, assessed using a standard rotarod test, is not significantly different from vehicle-treated cohorts. Finally, although there is minor group-to-group variability, there are no significant differences in white blood cell counts or neutrophil content between any of the treatment cohorts. Thus the low doses of Epothilone D (EpoD) utilized in these studies appeared to be well tolerated. |
Last Update：2024-04-09 19:05:05
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Product Name: Oxacyclohexadec-13-ene-2,6-dione, 4,8-dihydroxy-5,5,7,9,13-pentamethyl-16-(1E)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl-, (4S,7R,8S,9S,13Z,16S)- Visit Supplier Webpage Request for quotation
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CAS: 189453-10-9
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