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Patupilone (Epothilone B)
Catalog No.S1364 Synonyms: EPO906
For research use only.
Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.
CAS No. 152044-54-7
Selleck's Patupilone (Epothilone B) has been cited by 13 publications
Purity & Quality Control
Choose Selective Microtubule Associated Inhibitors
Related Compound Libraries
Other Microtubule Associated Products
Biological Activity
| Description | Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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 (from reference)
| Kinase Assay:[1] |
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| Cell Research:[2] |
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| Animal Research:[4] |
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| References |
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Solubility (25°C)
|
In vitro |
DMSO |
102 mg/mL
(200.91 mM) |
| Ethanol |
102 mg/mL
(200.91 mM) |
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| Water |
Insoluble
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In vivo |
Add solvents to the product individually and in order |
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 | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| 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)
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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
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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.
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 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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