1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin

Epothilone B (Synonyms: EPO 906; Patupilone)

Cat. No.: HY-17029 Purity: 99.78%
Data Sheet SDS Handling Instructions

Epothilone B is a microtubule (MT) targeting agent with EC0.01 of 1.8 μM.

For research use only. We do not sell to patients.
Epothilone B Chemical Structure

Epothilone B Chemical Structure

CAS No. : 152044-54-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO $78 In-stock
2 mg $50 In-stock
5 mg $70 In-stock
10 mg $116 In-stock
50 mg $415 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Epothilone B is a microtubule (MT) targeting agent with EC0.01 of 1.8 μM.

IC50 & Target

EC0.01: 1.8 μM (Microtubule/Tubulin)[1]

In Vitro

Epothilone B inhibits HCT116 cells with IC50 of 0.8 nM in HCT-116 cell line cytotoxicity assay[1]. Epothilone B (Patupilone) is a microtubule (MT) targeting agent. As shown by MTT cell proliferation assay, after 72 h of treatment Epothilone B efficiently inhibits cell growth with an IC50 of 6 nM, while concentrations ≤1 nM are not cytotoxic. Epothilone B significantly inhibits transwell cell migration at the non-cytotoxic concentration of 1 nM, and the effect is more evident at 10 nM[2]. Epothilone B (Patupilone) is a novel, non-taxane-related and nonneurotoxic microtubule-stabilizing agent in human medulloblastoma cell lines. Epothilone B reduces the proliferative activity in the D341 cell line, with an IC50 of 0.53 nM; in the D425Med cell line, with an IC50 of 0.37 nM; and in the DAOY cell line, with an IC50 of 0.19 nM. In the D341Med cell line, the effect of Epothilone B on clonogenic survival is at dose range of Epothilone B similar to the level of proliferative activity and viability (IC50, 0.50-0.75 nM). However, the clonogenicity of D425Med and DAOY cells is already strongly reduced at a 10-fold lower concentration of Epothilone B (IC50, 30 pM). These results overall demonstrate that Epothilone B is highly potent against different medulloblastoma cell lines[3].

In Vivo

Treatment with Epothilone B (Patupilone) or ionizing radiation alone results in a partial tumor growth suppression over 10 days, whereas combined treatment exerts a strong supra-additive tumor growth control, with complete tumor regression in the follow-up period (P<0.005, for ionizing radiation or Epothilone B alone vs combined treatment)[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00450866 David Peereboom, MD|National Cancer Institute (NCI)|Case Comprehensive Cancer Center Breast Cancer|Metastatic Cancer January 2007 Phase 2
NCT00035100 Novartis Pharmaceuticals|Novartis Ovarian Neoplasms|Peritoneal Neoplasms|Fallopian Tube Neoplasms September 2001 Phase 2
NCT00035165 Novartis Pharmaceuticals|Novartis Melanoma March 2002 Phase 2
NCT00050349 Novartis Pharmaceuticals|Novartis Carcinoid|Neuroendocrine Tumors July 2002 Phase 2
NCT00035243 Novartis Pharmaceuticals|Novartis Kidney Neoplasms April 2002 Phase 2
NCT00328458 Thomas Jefferson University|Novartis Pharmaceuticals Central Nervous System Neoplasms|Head and Neck Neoplasms February 2004 Phase 1
NCT00035126 Novartis Pharmaceuticals|Novartis Breast Neoplasms January 2002 Phase 2
NCT00035087 Novartis Pharmaceuticals|Novartis Colorectal Neoplasms|Colonic Neoplasms May 2002 Phase 2
NCT00035113 Novartis Pharmaceuticals|Novartis Prostatic Neoplasms January 2002 Phase 2
NCT00420615 Novartis Pharmaceuticals|Novartis Solid Tumors December 2006 Phase 1
NCT00412789 Novartis Pharmaceuticals|Novartis Tumors August 2006 Phase 1
NCT00262990 Novartis Pharmaceuticals|Novartis Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Neoplasms November 2005 Phase 3
NCT00273312 Novartis Pharmaceuticals|Novartis Hepatocellular Carcinoma January 2006 Phase 2
NCT00448396 Novartis Pharmaceuticals|Novartis Advanced Malignancies March 2007 Phase 1
NCT00426582 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors August 2006 Phase 1
NCT00426140 Novartis Pharmaceuticals|Novartis Advanced Malignancies|Solid Tumors August 2006 Phase 1
NCT00442741 Novartis Pharmaceuticals|Novartis Solid Tumors July 2007 Phase 1
NCT00496600 University of Medicine and Dentistry of New Jersey|Novartis Pharmaceuticals|National Cancer Institute (NCI)|Rutgers, The State University of New Jersey Refractory Malignancy July 2007 Phase 1
NCT00171834 Novartis Pharmaceuticals|Novartis Carcinoma, Non-Small-Cell Lung August 2003 Phase 1|Phase 2
NCT00420524 Novartis Pharmaceuticals|Novartis Advanced Malignancies|Tumors January 2006 Phase 1
NCT00468260 Novartis Pharmaceuticals|Novartis Advanced Malignancies May 2007 Phase 1
NCT00715013 University of Zurich Recurrent Glioblastoma Planned for Reoperation July 2008 Phase 1|Phase 2
NCT00219297 Novartis Pharmaceuticals|Novartis Brain Metastasis|Non-small Cell Lung Cancer November 2005 Phase 2
NCT00411528 Novartis Pharmaceuticals|Novartis Metastatic Hormone Refractory Prostate Cancer September 2006 Phase 2
NCT00421044 Novartis Pharmaceuticals|Novartis Advanced Malignancies|Tumors May 2006 Phase 1
NCT00407251 British Columbia Cancer Agency Hormone Refractory Prostate Cancer February 2007 Phase 2
NCT00969046 Novartis Pharmaceuticals|Novartis Colon Cancer November 2003 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.9697 mL 9.8487 mL 19.6974 mL
5 mM 0.3939 mL 1.9697 mL 3.9395 mL
10 mM 0.1970 mL 0.9849 mL 1.9697 mL
Kinase Assay
[3]

Asp-Glu-Val-Asp (DEVD)ase activity is determined in cytosolic cell extracts. Cells are treated with increasing concentrations of Epothilone B (Patupilone) for 6, 12, 24, and 48 h. Cells are harvested thereafter by trypsin/EDTA, centrifuged, and washed with precooled PBS. The cell pellet is suspended in 5 volumes of precooled buffer A (20 mM HEPES-KOH [pH 7.5], 10 mM KCl, 1.5 mM MgCl2, 1 mM sodium EDTA, 1 mM sodium EGTA, 1 mM dithiothreitol [DDT], 250 mM sucrose, and 0.1 mM phenylmethylsulfonyl fluoride [PMSF] supplemented with protease inhibitors [5 mg/mL pepstatin A, 10 mg/mL leupeptin, 2 mg/mL aprotinin, 2 mg/mL DTT, and 1 mM of PMSF]). After incubation on ice for 15 min, the cells are disrupted by freezing and thawing. Cell lysates are centrifuged at 1000g for 10 min at 4°C, and the supernatant is further centrifuged at 100 000g for 30 min. The resulting supernatant (S-100 fraction) is stored at −80°C. To determine caspase 3-like activity, 75 μg of protein from the S-100 fraction is incubated at 37°C with the colorimetric caspase 3 substrate N-acetyl-Asp-Glu-Val-Asp p-nitroanilide (100 mM; Ac-DEVD-pNA) and 1 mM dATP in a final volume of 120 μL. Cleavage of the caspase substrate is monitored at 405 nm using a GenTec spectrophotometer[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

Epothilone B (Patupilone) is dissolved in DMSO and then diluted (10 μM)[2].

Human glioblastoma cells (U87MG, ATCC) are routinely maintained at 37°C and 5% CO2 in EMEM medium, with NEAA, containing 10% fetal bovine serum, 2 mM of glutamine, 1% penicillin and streptomycin. U87MG cells are used for no more than 15 passages. Cells are seeded in 96-well plates (5000 cells/well). After 24 h cells are treated with Epothilone B. Growth inhibition of U87MG cells is measured after 72 h of drug treatment by using the MTT cell proliferation assay[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Epothilone B (Patupilone) is dissolved in 30% PEG-300/70% saline (Mice)[3].

Mice[3]
D425Med cells (6×106) are injected subcutaneously on the backs of 4-6-week-old athymic nude mice. Tumor volumes are determined from caliper measurements of tumor length (L) and width (l) according to the formula (L×l2)/2. Tumors are allowed to expand to a volume of 200 mm3 (±10%) before treatment start. With the use of a customized shielding device, mice are given strictly loco regional radiotherapy of 3×3 Gy on 3 consecutive days using a Gulmay 200 kV X-ray unit at 100 cGy/min at room temperature. Epothilone B (2 mg/kg; dissolved in 30% PEG-300/70% saline) is applied intravenously 24 h before the first treatment with ionizing radiation (at day 0 of the treatment; n=5 per group). Tumor growth is monitored daily. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
M.Wt

507.68

Formula

C₂₇H₄₁NO₆S

CAS No.

152044-54-7

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Epothilone B
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