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In vitro: 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: 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 (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 or vehicle. The 3 mg/kg Epothilone D 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 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-treated mice. The motor performance of Epothilone D-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 utilized in these studies appeared to be well tolerated.
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Mice |
| Formulation | dissolved in 100% DMSO and diluted with saline or PBS |
| Dosages | 3 mg/kg |
| Administration | i.p. |
| Molecular Weight | 491.68 |
| Formula | C27H41NO5S |
| CAS Number | 189453-10-9 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Microtubule Products |
|---|
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Nab-Paclitaxel (Nanoparticle albumin-bound Paclitaxel) is an albumin-bound nanoparticle formulation of Paclitaxel. Nab-Paclitaxel is composed of albumin and the active pharmaceutical ingredient Paclitaxel, in which human albumin is used as an excipient to disperse and stabilize particles and carry the main drug. Nab-Paclitaxel is a solvent-free taxane with higher response rates and improved tolerability. Nab-Paclitaxel displays less toxicity and greater antitumor activity. |
| CCB02
CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC50 of 689 nM, and shows potent anti-tumor activity. |
| Lisavanbulin
Lisavanbulin (BAL-101553) is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862). |
| 20-O-Demethyl-AP3
20-O-Demethyl-AP3 is a minor metabolite of Ansamitocin P-3. |
| Lisavanbulin dihydrochloride
Lisavanbulin (BAL-101553) dihydrochloride is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862). |
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