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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Matrigel invasion assay of H1299 cells treated with SDF-1α or SDF-1α plus Epothilone B prior to 0 or 2 Gy irradiation. After the treatment for 12 h, the H1299 cells that migrated to the bottom surface of the membrane were stained with Giemsa, and the number of migrated cells was calculated manually.
Oncotarget, 2015, 6(13):10893-907.. Patupilone (EPO906, Epothilone B) purchased from Selleck.
Combination treatment with epothilone B and ABT-737 inhibited PI3K/AKT/mTOR pathway. SKOV-3 cells were treated with epothilone B (0.4 nM), ABT-737 (5 μM), or the combination, OVCAR-8 cells were treated with epothilone B (0.3 nM), ABT-737 (3 μM), or the combination, SGC-7901 were treated with epothilone B (0.4 nM), ABT-737 (5 μM), or the combination. Cells were exposed to compounds for 48 h, after which protein extracts were immunoblotted with specified antibodies for p-4E-BP-1, p-mTOR, p-AKT, caspase-3, PARP and β-actin.
J Cancer Res Clin Oncol, 2016, 142(11):2281-9.. Patupilone (EPO906, Epothilone B) purchased from Selleck.
Purity & Quality Control
Choose Selective Microtubule Associated Inhibitors
|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||Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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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|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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