Patupilone (EPO906, Epothilone B)
Molecular Weight(MW): 507.68
Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.
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|Description||Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.|
Epothilone B shows better activity than Epothilone A. The EC0.01 of Epothilone B is 1.8 μM. Epothilone B potently inhibits cell proliferation in HCT116 cells, with IC50 of 0.8 nM.  Epothilone B induces mitotic arrest and displays cytotoxicity in KB3-1, KBV-1, Hela, and Hs578T cells, with IC50 of 3 nM to 92 nM. Epothilone B competes with Taxol in binding to microtubules, with IC50 of 3.3 μM.  In MCF-7 cells overexpressing GFP-α-tubulin, Epothilone B (3.5 nM) efficiently blocks microtubule dynamics. Meanwhile, Epothilone B induces mitotic arrest with IC50 of 3.5 nM.  In multiple myeloma (MM) cells, including RPMI 8226, U266, MM.1S, LR5, and MR20, Epothilone B directly suppresses proliferation with IC50 of 1 nM to 10 nM. Similarly, Epothilone B (10 nM) also induces cell cycle arrest and apoptosis.  A recent study reveals that, in ovarian cancer Hey cells, Epothilone B (5 nM–100 nM) enhances surface epithelial cell adhesion antigen (EpCAM), without affecting the transcription or the total cellular level of EpCAM. 
|In vivo||In a mouse xenograft model of RPMI 8226 cells, Epothilone B (2.5 mg/kg–4 mg/kg) prolongs survival and suppresses tumor growth.  Similarly, in mouse xenograft models of prostate cancer cells, including DU145 and PC3, Epothilone B at the same dose also inhibits tumor growth. |
Tubulin polymerization assay:Calf brain microtubule proteins (MTP) are purified, which includes approximately 15%–20% microtubule associated proteins. The buffer (MES buffer) used for the Epothilone B-microtubule studies contains 0.1 M 2-morpholinoethanesulfonic acid (MES), 1 mM EGTA, 0.5 mM MgCl2, and 3 M glycerol at pH 6.6. Samples for electron microscopy are placed on carbon-over-Parlodion-coated grids (300 mesh) and negatively stained with 2% uranyl acetate. Microtubule assembly in the presence or absence of Epothilone B is monitored spectrophotometrically by using a spectrophotometer equipped with a thermostatically regulated liquid circulator. The temperature is held at 35 °C and changes in turbidity (representative of polymer mass) are monitored at 350 nm. Effective concentration (EC0.01), defined as the interpolated concentration capable of inducing an initial slope of 0.01 OD/min rate, is calculated using the formula EC0.01 = concentration/slope and expressed as the mean with standard deviation obtained from three different concentrations.
-  Regueiro-Ren A , et al. Org Lett, 2001, 3(17), 2693-2696.
-  Bollag DM, et al. Cancer Res, 1995, 55(11), 2325-2333.
-  Kamath K, et al. Cancer Res, 2003, 63(18), 6026-6031.
|In vitro||DMSO||102 mg/mL (200.91 mM)|
|Ethanol||102 mg/mL (200.91 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||5 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00715013||Completed||Recurrent Glioblastoma Planned for Reoperation||University of Zurich||July 2008||Phase 1|Phase 2|
|NCT00442741||Withdrawn||Solid Tumors||Novartis Pharmaceuticals|Novartis||July 2007||Phase 1|
|NCT00496600||Completed||Refractory Malignancy||University of Medicine and Dentistry of New Jersey|Novartis Pharmaceuticals|National Cancer Institute (NCI)|Rutgers, The State University of New Jersey||July 2007||Phase 1|
|NCT00468260||Terminated||Advanced Malignancies||Novartis Pharmaceuticals|Novartis||May 2007||Phase 1|
|NCT00448396||Completed||Advanced Malignancies||Novartis Pharmaceuticals|Novartis||March 2007||Phase 1|
|NCT00407251||Completed||Hormone Refractory Prostate Cancer||British Columbia Cancer Agency||February 2007||Phase 2|
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