Patupilone (Epothilone B)
For research use only.
Catalog No.S1364 Synonyms: EPO906
11 publications
CAS No. 152044-54-7
Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.
4 Customer Reviews
-
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 (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 (Epothilone B) 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. Patupilone (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 (Epothilone B) purchased from Selleck.
Purity & Quality Control
Choose Selective Microtubule Associated Inhibitors
Biological Activity
| Description | Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 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] |
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Cell Data |
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 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:[1] |
- Collapse
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:[2] |
- Collapse
|
| Animal Research:[4] |
- Collapse
|
Solubility (25°C)
| In vitro | DMSO | 102 mg/mL (200.91 mM) |
|---|---|---|
| Ethanol | 102 mg/mL (200.91 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% PEG400+0.5% Tween80+5% propylene glycol For best results, use promptly after mixing. |
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.
Chemical Information
| Molecular Weight | 507.68 |
|---|---|
| Formula | C27H41NO6S |
| CAS No. | 152044-54-7 |
| Storage |
powder in 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 |
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 | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT00496600 | Completed | Drug: Patupilone|Drug: RAD001 | 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 | Drug: Patupilone|Drug: Patupilone + Omeprazole | Solid Tumors | Novartis Pharmaceuticals|Novartis | July 2007 | Phase 1 |
| NCT00468260 | Terminated | Drug: Patupilone | Advanced Malignancies | Novartis Pharmaceuticals|Novartis | May 2007 | Phase 1 |
| NCT00448396 | Completed | Drug: Patupilone | Advanced Malignancies | Novartis Pharmaceuticals|Novartis | March 2007 | Phase 1 |
| NCT00426140 | Completed | Drug: Patupilone | Advanced Malignancies|Solid Tumors | Novartis Pharmaceuticals|Novartis | August 2006 | Phase 1 |
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
