Home Cytoskeletal Signaling Microtubule Associated inhibitor Patupilone (Epothilone B) For research use only.

Patupilone (Epothilone B)

Synonyms: EPO906

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

Patupilone (Epothilone B) Chemical Structure

Patupilone (Epothilone B) Chemical Structure

CAS No. 152044-54-7

Purity & Quality Control

Patupilone (Epothilone B) Related Products

Signaling Pathway

Microtubule Associated Signaling Pathways

Microtubule Associated Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human LC-2-ad cell Growth inhibition assay Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=3.77e-06 μM SANGER
human A431 cell Growth inhibition assay Inhibition of human A431 cell growth in a cell viability assay, IC50=9.86e-06 μM SANGER
human SW1710 cell Growth inhibition assay Inhibition of human SW1710 cell growth in a cell viability assay, IC50=2.14e-05 μM SANGER
human Daoy cell Growth inhibition assay Inhibition of human Daoy cell growth in a cell viability assay， IC50=2.73e-05 μM SANGER
human BFTC-905 cell Growth inhibition assay Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=4.99e-05 μM SANGER
human A375 cell Growth inhibition assay Inhibition of human A375 cell growth in a cell viability assay, IC50=5e-05 μM SANGER
human RKO cell Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=6.47e-05 μM SANGER
human KYSE-510 cell Growth inhibition assay Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50=7.38e-05 μM SANGER
human HLE cell Growth inhibition assay Inhibition of human HLE cell growth in a cell viability assay, IC50=8.26e-05 μM SANGER
human MCF7 cell Growth inhibition assay Inhibition of human MCF7 cell growth in a cell viability assay, IC50=8.66e-05 μM SANGER
human 786-0 cell Growth inhibition assay Inhibition of human 786-0 cell growth in a cell viability assay, IC50=0.11 nM SANGER
human TE-8 cell Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=0.111 nM SANGER
ovarian carcinoma 1A9 cell Growth inhibition assay Inhibitory concentration against ovarian carcinoma 1A9 cell growth 16134928
human PANC-03-27 cell Growth inhibition assay Inhibition of human PANC-03-27 cell growth in a cell viability assay, IC50=0.132 μM SANGER
human VMRC-RCZ cell Growth inhibition assay Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50=0.136 μM SANGER
human IGROV-1 cell Growth inhibition assay Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=0.156 μM SANGER
human MG-63 cell Growth inhibition assay Inhibition of human MG-63 cell growth in a cell viability assay, IC50=0.165 μM SANGER
human SIG-M5 cell Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=0.169 μM SANGER
human NCI-H650 cell Growth inhibition assay Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=0.17 μM SANGER
human PSN1 cell Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50=0.173 μM SANGER
human PA-1 cell Growth inhibition assay Inhibition of human PA-1 cell growth in a cell viability assay, IC50=0.174 μM SANGER
KB-8511 cells Growth inhibition assay 72 h Concentration required to inhibit the growth of human epidermoid carcinoma cells KB-8511 by 50 percent (72 hr exposure), IC50=0.18 μM 11133086
KB-31 cells Growth inhibition assay 72 h Concentration required to inhibit the growth of human epidermoid carcinoma cells KB-31 by 50 percent (72 hr exposure) 11133086
human BHY cell Growth inhibition assay Inhibition of human BHY cell growth in a cell viability assay, IC50=0.195 nM SANGER
human BB30-HNC cell Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=0.201 μM SANGER
human HOS cell Growth inhibition assay Inhibition of human HOS cell growth in a cell viability assay, IC50=0.215 μM SANGER
human 639-V cell Growth inhibition assay Inhibition of human 639-V cell growth in a cell viability assay, IC50=0.218 μM SANGER
human ES1 cell  Growth inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50=0.221 μM SANGER
human TE-15 cell  Growth inhibition assay Inhibition of human TE-15 cell growth in a cell viability assay, IC50=0.225 μM SANGER
human LXF-289 cell Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=0.277 μM SANGER
human CAL-12T cell Growth inhibition assay Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=0.239 μM SANGER
human T84 cell Growth inhibition assay Inhibition of human T84 cell growth in a cell viability assay, IC50=0.24 μM SANGER
human KYSE-450 cell Growth inhibition assay Inhibition of human KYSE-450 cell growth in a cell viability assay, IC50=0.267 μM SANGER
human LCLC-103H cell Growth inhibition assay Inhibition of human LCLC-103H cell growth in a cell viability assay, IC50=0.31 nM SANGER
human NCI-H810 cell Growth inhibition assay Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=0.322 μM SANGER
human HUTU-80 cell Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=0.328 μM SANGER
human NCI-H460 cell Growth inhibition assay Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=0.333 μM SANGER
human HGC-27 cell Growth inhibition assay Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=0.338 μM SANGER
human HSC-2 cell Growth inhibition assay Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=0.363 nM SANGER
human IA-LM cell Growth inhibition assay Inhibition of human IA-LM cell growth in a cell viability assay, IC50=0.393 μM SANGER
human HMV-II cell Growth inhibition assay Inhibition of human HMV-II cell growth in a cell viability assay, IC50=0.394 μM SANGER
human COLO-679 cell Growth inhibition assay Inhibition of human COLO-679 cell growth in a cell viability assay, IC50=0.394 μM SANGER
human NCI-H2122 cell Growth inhibition assay Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=0.41 μM SANGER
human CAL-39 cell Growth inhibition assay Inhibition of human CAL-39 cell growth in a cell viability assay, IC50=0.411 μM SANGER
human SW954 cell Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay, IC50=0.436 μM SANGER
human LCLC-97TM1 cell Growth inhibition assay Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=0.444 μM SANGER
human KYSE-270 cell Growth inhibition assay Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50=0.445 μM SANGER
human NB13 cell Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay, IC50=0.447 μM SANGER
human SK-LMS-1 cell Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=0.646 μM SANGER
human SW620 cell Growth inhibition assay Inhibition of human SW620 cell growth in a cell viability assay, IC50=0.648 μM SANGER
human HCT-15 cell Growth inhibition assay Inhibition of human HCT-15 cell growth in a cell viability assay, IC50=0.717 μM SANGER
human DU-145 cell Growth inhibition assay Inhibition of human DU-145 cell growth in a cell viability assay, IC50=0.721 μM SANGER
human ST486 cell Growth inhibition assay Inhibition of human ST486 cell growth in a cell viability assay, IC50=0.721 μM SANGER
human A427 cell Growth inhibition assay Inhibition of human A427 cell growth in a cell viability assay, IC50=0.828 μM SANGER
human HT-1080 cell Growth inhibition assay Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=0.842 μM SANGER
human NCI-H2009 cell Growth inhibition assay Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=0.862 μM SANGER
human SK-LU-1 cell Growth inhibition assay Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=0.866 μM SANGER
human SCC-4 cell Growth inhibition assay Inhibition of human SCC-4 cell growth in a cell viability assay, IC50=0.877 μM SANGER
human NCI-H1299 cell Growth inhibition assay Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=0.88 μM SANGER
human NH-12 cell Growth inhibition assay Inhibition of human NH-12 cell growth in a cell viability assay, IC50=0.891 μM SANGER
human SK-UT-1 cell Growth inhibition assay Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=0.892 μM SANGER
human Bel7402 Proliferation assay 72 h Antiproliferative activity against human Bel7402 after 72 hrs by CellTiter Glo assay, IC50=0.9 μM 22320354
human A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=0.94 μM SANGER
human SW982 cell Growth inhibition assay Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.999 μM SANGER
Click to View More Cell Line Experimental Data

Biological Activity

Description Patupilone (EPO906, Epothilone B) is a 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
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]
Kinase Assay 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 and 0.5 mM MgCl2 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 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 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 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.
In Vivo
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]
Animal Research Animal Models Mice xenograft model of RPMI 8226 cells
Dosages 2.5 mg/kg–4 mg/kg
Administration Inject intravenously
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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
NCT00442741 Withdrawn
Solid Tumors
Novartis Pharmaceuticals|Novartis
 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
NCT00426140 Completed
Advanced Malignancies|Solid Tumors
Novartis Pharmaceuticals|Novartis
 August 2006 Phase 1

Chemical Information & Solubility

Molecular Weight 507.68 Formula

C27H41NO6S
CAS No. 152044-54-7 SDF Download Patupilone (Epothilone B) SDF
Smiles CC1CCCC2(C(O2)CC(OC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 102 mg/mL ( (200.91 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 102 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Patupilone (Epothilone B) | Patupilone (Epothilone B) supplier | purchase Patupilone (Epothilone B) | Patupilone (Epothilone B) cost | Patupilone (Epothilone B) manufacturer | order Patupilone (Epothilone B) | Patupilone (Epothilone B) distributor