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IC50: 2.9 nM for MCF-7 cell line; 2.7 nM for KB-31 cell line; 9.5 nM for CCRF-CEM cell line

Drugs targeting tubulin are active in human malignant disease and are an essential component of medical treatment of these diseases. As a result, pharmaceutical research on compounds that interfere with tubulin function has concentrated on agents which might have enhanced efficacy or reduced toxicity. Epothilone D is a more potent microtubule stabilizer.

In vitro: Epothilone D is a more potent microtubule stabilizer in vitro than epothilone A or B. In vitro, Epothilone D showed potent cytotoxicity in a panel of human tumor cell lines, with similar potency to paclitaxel. It also showed definite advantage over paclitaxel in drug-resistant cell lines, and retained its cytotoxicity against a multidrug resistant cell line over-expressing P-glycoprotein [1].

In vivo: In vivo, antitumor efficacy of Epothilone D has been observed in both paclitaxel sensitive and resistant xenografts, as well as certain multidrug resistant xenografts including a doxorubinresistant CCRF-CEM leukemic cell xenograft [1].

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