Epothilone B (EPO906, Patupilone)

Catalog No.S1364

Epothilone B (EPO906, Patupilone) Chemical Structure

Molecular Weight(MW): 507.68

Epothilone B (EPO906, Patupilone) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.

Size Price Stock Quantity  
In DMSO USD 250 In stock
USD 70 In stock
USD 120 In stock
USD 210 In stock
USD 470 In stock

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3 Customer Reviews

  • Oncotarget, 2015, 6(13):10893-907.. Epothilone B (EPO906, Patupilone) purchased from Selleck.

    J Cancer Res Clin Oncol, 2016, 142(11):2281-9.. Epothilone B (EPO906, Patupilone) purchased from Selleck.

  • Cells were seeded in 96 well paltes, and then treated with the indicated concentration of Epothilone B for 48 h. Cell survival was measured by a standarad MTT assay.

     

     

    Dr. Helen Sadik of Johns Hopkins University. Epothilone B (EPO906, Patupilone) purchased from Selleck.

Purity & Quality Control

Choose Selective Microtubule Associated Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Epothilone B (EPO906, Patupilone) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.
Targets
Tubulin [1]
(Cell-free assay)
1.8 μM(EC0.01)
In vitro

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. [1] 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. [2] 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. [3] 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. [4] 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. [5]

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. [4] Similarly, in mouse xenograft models of prostate cancer cells, including DU145 and PC3, Epothilone B at the same dose also inhibits tumor growth. [6]

Protocol

Kinase Assay
+ Expand

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.
Cell Research
+ Expand
  • Cell lines: KB3-1, KBV-1, Hela, and Hs578T cells
  • Concentrations: 0–1 μM
  • Incubation Time: 72 hours
  • Method: For mitotic block and aberrant mitosis, cells are plated either in 48-well plates (for trypan blue and cell counting) or onto coverslips. After 24 hours, cells are treated with Epothilone B and scored at regular intervals. For the cytotoxicity analysis, cells are counted and scored as trypan blue positive or negative. Concurrently, coverslips andaliquots of cells in the culture supernatant are fixed and stained with Hoechst33342 in PBS. These cells are scored for cells blocked at the G2/M transition and aberrant mitosis.
    (Only for Reference)
Animal Research
+ Expand
  • Animal Models: Mice xenograft model of RPMI 8226 cells
  • Formulation: Dissolved in30% PEG-300
  • Dosages: 2.5 mg/kg–4 mg/kg
  • Administration: Inject intravenously
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 102 mg/mL (200.91 mM)
Ethanol 102 mg/mL (200.91 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 5 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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.

Chemical Information

Molecular Weight 507.68
Formula

C27H41NO6S

CAS No. 152044-54-7
Storage powder
in solvent
Synonyms N/A

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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

Tech Support

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Microtubule Associated Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID