Epothilone B (EPO906, Patupilone)

Catalog No.S1364
1 Reviews

Epothilone B is a Taxol-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.

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Epothilone B (EPO906, Patupilone) Chemical Structure

Epothilone B (EPO906, Patupilone) Chemical Structure
Molecular Weight: 507.68

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

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Epothilone B (EPO906, Patupilone) is available in the following compound libraries:

Product Information

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  • Epothilone B (EPO906, Patupilone) Mechanism

Product Description

Biological Activity

Description Epothilone B is a Taxol-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.
Targets Tubulin
IC50 1.8 μM (EC0.01) [1]
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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [2]

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.

Animal Study: [4]

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
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, 5 mg/mL
* 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.
1

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01084057 Active, not recruiting Male Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer City of Hope Medical Center 2010-05 Phase 1
NCT01168232 Active, not recruiting Recurrent Uterine Sarcoma|Uterine Carcinosarcoma National Cancer Institute (NCI) 2010-09 Phase 2
NCT01220609 Active, not recruiting Recurrent Uterine Sarcoma|Uterine Leiomyosarcoma National Cancer Institute (NCI) 2010-11 Phase 2
NCT01454479 Enrolling by invitation Recurrent Endometrial Cancer Chang Gung Memorial Hospital|Hung-Hsueh Chou|GlaxoSmithKline|Bristol-Myers Squibb 2011-03 Phase 1
NCT01375829 Recruiting Unspecified Adult Solid Tumor, Protocol Specific National Cancer Institute (NCI) 2011-06 Phase 1

Chemical Information

Download Epothilone B (EPO906, Patupilone) SDF
Molecular Weight (MW) 507.68
Formula

C27H41NO6S

CAS No. 152044-54-7
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 102 mg/mL (200 mM)
Water <1 mg/mL (<1 mM)
Ethanol 102 mg/mL (200 mM)
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 Name (1S,3S,7S,10R,11S,12S,16R,E)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-(1-(2-methylthiazol-4-yl)prop-1-en-2-yl)-4,17-dioxa-bicyclo[14.1.0]heptadecane-5,9-dione

Research Area

Customer Reviews (1)


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Rating
Source Dr. Helen Sadik of Johns Hopkins University. Epothilone B (EPO906, Patupilone) purchased from Selleck
Method MTT assays
Cell Lines MCF7 cells, MCF10A cells
Concentrations 1-100000 nM
Incubation Time 48 h
Results Epothilone B potently inhibited the survival of MCF10A cells and MCF7 cells in a dose-dependent manner.

Tech Support & FAQs

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