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Patupilone (Epothilone B) Microtubule Associated inhibitor

Name: Patupilone (Epothilone B)
Brand: Selleck Chemicals
SKU: S1364
Availability: InStock
Rating: 5 (17 reviews)

Cat.No.S1364

Patupilone (EPO906, Epothilone B) is a microtubule-stabilizing agent with EC_0.01 of 1.8 μM, currently in Phase 2.

Chemical Structure

Molecular Weight: 507.68

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Akt Wnt/beta-catenin HSP PKC ROCK Integrin Bcr-Abl Actin FAK Kinesin
Other Microtubule Associated Inhibitors	Nocodazole MMAF Lexibulin (CYT997) CW069 Combretastatin A4 ABT-751 (E7010) Epothilone A Cucurbitacin B TAI-1 Vindoline

Cell Culture, Treatment & Working Concentration

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

Solubility

In vitro
Batch:

DMSO : 102 mg/mL (200.91 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 102 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.85mM)	Taking the 1 mL working solution as an example, add 300 μL of 16.67 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O Dilute to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	507.68	Formula	C₂₇H₄₁NO₆S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	152044-54-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	EPO906			Smiles	CC1CCCC2(C(O2)CC(OC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C)C

Mechanism of Action

Targets/IC₅₀/Ki	Tubulin (Cell-free assay) 1.8 μM(EC0.01)
In vitro	Patupilone (Epothilone B) shows better activity than Epothilone A, with an EC_0.01 of 1.8 μM. It potently inhibits cell proliferation in HCT116 cells, with IC50 of 0.8 nM. This compound induces mitotic arrest and displays cytotoxicity in KB3-1, KBV-1, Hela, and Hs578T cells, with IC50 of 3 nM to 92 nM. It competes with Taxol in binding to microtubules, with IC50 of 3.3 μM. In MCF-7 cells overexpressing GFP-α-tubulin, it (3.5 nM) efficiently blocks microtubule dynamics. Meanwhile, it induces mitotic arrest with IC50 of 3.5 nM. In multiple myeloma (MM) cells, including RPMI 8226, U266, MM.1S, LR5, and MR20, it directly suppresses proliferation with IC50 of 1 nM to 10 nM. Similarly, it (10 nM) also induces cell cycle arrest and apoptosis. A recent study reveals that, in ovarian cancer Hey cells, it (5 nM–100 nM) enhances surface epithelial cell adhesion antigen (EpCAM), without affecting the transcription or the total cellular level of EpCAM.
Kinase Assay	Tubulin polymerization assay
Kinase 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 Patupilone (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 (EC_0.01), defined as the interpolated concentration capable of inducing an initial slope of 0.01 OD/min rate, is calculated using the formula EC_0.01 = concentration/slope and expressed as the mean with standard deviation obtained from three different concentrations.
In vivo	In a mouse xenograft model of RPMI 8226 cells, Patupilone (Epothilone B) (2.5 mg/kg–4 mg/kg) prolongs survival and suppresses tumor growth. Similarly, this compound at the same dose also inhibits tumor growth in mouse xenograft models of prostate cancer cells, including DU145 and PC3.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11506611/ [2] https://pubmed.ncbi.nlm.nih.gov/7757983/ [3] https://pubmed.ncbi.nlm.nih.gov/14522931/ [4] https://pubmed.ncbi.nlm.nih.gov/15367426/ [5] https://pubmed.ncbi.nlm.nih.gov/20674962/ [6] https://pubmed.ncbi.nlm.nih.gov/15948135/ [7] https://pubmed.ncbi.nlm.nih.gov/1672157/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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