Chemren Bio-Engineering Co., Ltd.

Epothilone D(Desoxyepothilone B; KOS 862) is a natural polyketide compound isolated from the myxobacterium Sorangium cellulosum.
IC50 Value:
Target: Microtubule/Tubulin
Epothilone D binds to tubulin and inhibits the disassembly of microtubules, resulting in the inhibition of mitosis, cellular proliferation, and cell motility. Intermediary obtained in the synthesis of members of the Epothilone family, polyketide natural products that inhibit cancer cells via a mechanism similar to Paclitaxel. Epothilone D also found to be effective against Paclitaxel-resistant tumors. Epothilone D currently in Phase I of clinical testing.

[1]. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy By Brunden, Kurt R.; Zhang, Bin; Carroll, Jenna; Yao, Yuemang; Potuzak, Justin S.; Hogan, Anne-Marie L.; Iba, Michiyo; James, Michael J.; X The Journal of Neuroscience, 13 October 2010, 30(41): 13861-13866;

[2]. Novel microtubule-targeting agents - the epothilones By Cheng, Kit L.; Bradley, Thomas; Budman, Daniel R.From Biologics: Targets & Therapy (2008), 2(4), 789-811.

[3]. Konner J, Grisham RN, Park J, O'Connor OA, Cropp G, Johnson R, Hannah AL, Hensley ML, Sabbatini P, Miranov S, Danishefsky S, Hyman D, Spriggs DR, Dupont J, Aghajanian CPhase I clinical, pharmacokinetic, and pharmacodynamic study of KOS-862 (Epothilone D) in patients with advanced solid tumors and lymphoma. Invest New Drugs. 2011 Nov 10.

[4]. Monk JP, Villalona-Calero M, Larkin J, Otterson G, Spriggs DS, Hannah AL, Cropp GF, Johnson RG, Hensley ML. A phase 1 study of KOS-862 (Epothilone D) co-administered with carboplatin (Paraplatin?) in patients with advanced solid tumors. Invest New Drugs. 2012 Aug;30(4):1676-83.

[5]. Brunden KR, Zhang B, Carroll J, Yao Y, Potuzak JS, Hogan AM, Iba M, James MJ, Xie SX, Ballatore C, Smith AB 3rd, Lee VM, Trojanowski JQ. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy. J Neurosci. 2010 Oct 13;30(41):13861-6.