Network Version
Epothilone D Data Sheet
| Product Name: | Epothilone D |
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|---|---|---|
| CAS No.: | 189453-10-9 | |
| Cat. No.: | HY-15278 | |
| MWt: | 491.68 | |
| Formula: | C27H41NO5S | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 100 mg/mL (203.38 mM) | |
| Mechanisms: | Target: Cancer Infection | |
| Biological Activity: | ||
| Epothilone D (KOS 862) is a potent microtubule stabilizer. IC50 & Target: Microtubule/Tubulin[1] 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[1]. Epothilone D (EpoD) is a microtubules (MTs)-stabilizing agent[2]. 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 (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[2]. | ||
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