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

Docetaxel 

Cat. No.: HY-B0011 Purity: 99.80%
Data Sheet SDS Handling Instructions

Docetaxel is a semi-synthetic taxane analogue, acts as a microtubule stabilizer.

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

Docetaxel Chemical Structure

CAS No. : 114977-28-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $66 In-stock
100 mg $60 In-stock
200 mg $85 In-stock
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Other Forms of Docetaxel:

    Docetaxel purchased from MCE. Usage Cited in: Oncotarget. 2016 May 17;7(20):28891-902.

    Western blot analyses for Brachyury and AR expression in prostate cell lines treated with Docetaxel (Doc) or with Cabazitaxel (Cab). Graphs represent the densimetric semi-quantification of western blot images.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Docetaxel is a semi-synthetic taxane analogue, acts as a microtubule stabilizer.

    IC50 & Target

    Microtubule[1]

    In Vitro

    Docetaxel (DOC) and Glufosfamide (GLU) single and combined treatments affect the cells viability in a dose-dependent manner. The IC50 of GLU are 70±4 µM and 86.8±8 µM in PC-3 and LNCaP cells; respectively. While, the IC50 of Docetaxel alone is found to be 3.08±0.4 nM and 1.46±0.2 nM in PC-3 and LNCaP cells; respectively. The co-treatment of GLU with Docetaxel is found to synergize the cytotoxicity and the IC50 values are decreased to be 2.7±0.1 nM and 0.75±0.3 nM in PC-3 and LNCaP cells; respectively[1]. IC50 of NCI-H460 to Docetaxel at 24 h is 116 nM and at 72 h is 30 nM. According to data reported in DTP Data Search, the mean IC50 of NCI-60 cell panel to Docetaxel is 14-34 nM[2].

    In Vivo

    In female mice, the Docetaxel-induced intestinal apoptosis in the 14-hours after light on (HALO) group is significantly greater than that in the 2-HALO group. Bax expression is significantly elevated by Docetaxel in the 2-HALO group, but not in the 14-HALO group. On the other hand, cleaved Caspase-3 expression is significantly elevated by Docetaxel in the 14-HALO group, but not in the 2-HALO group. The expressions of Wee1 and phosphorylated CKD1 are significantly elevated after dosing of Docetaxel at 14 HALO, but not at 2 HALO. In addition, Docetaxel significantly reduces survivin expression in the 14-HALO group but not in the 2-HALO group. The survivin expression level in the Docetaxel-treated 14-HALO group is significantly smaller than that in the drug-treated 2-HALO group[3]. Piperine (PIP) is administrated via intravenous bolus at 3.5 mg/kg and via oral administration at 35 mg/kg and 3.5 mg/kg, while Docetaxel (DOX) is intravenously administrated at 7 mg/kg to Sprague-Daley rats. The co-administrations of PIP at 35 mg/kg via oral administration and Docetaxel at 7 mg/kg via intravenous bolus administration in Sprague-Dawley rats. The combination use of PIP and Docetaxel results in a synergic increase of both their in vivo exposure[4].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.2378 mL 6.1890 mL 12.3781 mL
    5 mM 0.2476 mL 1.2378 mL 2.4756 mL
    10 mM 0.1238 mL 0.6189 mL 1.2378 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    Docetaxel is dissolved in DMSO (100 mM) and stored, and then diluted with appropriate media before use[1].

    Single-drug concentration-response curves are assessed. Seeding is done at a density of 2,000 cells/well for PC-3 and LNCaP, in 96-well plates. Cells are treated with each single drug and their combination for 72 h at different drug concentrations. Docetaxel is used at concentrations of 0.1-1,000 nM. GLU is used at concentrations of 0.1-300 µm. Cytotoxicity is assessed at the end of drug exposure using SRB assay. Following 72 h exposure the cells are fixed with 10% trichloroacetic acid (150 µL) for 1 h at 4°C. Then, cells are stained for 10 min at room temperature with 0.4% SRB dissolved in 1% acetic acid. The plates are then air dried for 24 h and the dye is made soluble with 150 µL Tris (10 mM, PH 7.4) for 5 min on a shaker at 1,600 rpm. Absorbance is then measured at 545 nM using microplate reader. Results are expressed as the relative percentage of absorbance compared to control[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    Docetaxel is dissolved in a solution to store 10 mg/mL and further diluted with saline just before each injection (Mice)[3].
    Docetaxel is dissolved in DMSO and then diluted with PEG 400, followed by saline (Rat)[4].

    Mice[3]
    Five-week-old male Balb/c mice are used. Docetaxel (0, 10, 20, 30, 40, 60, and 80 mg/kg per week) is given once a week for 3 weeks for mice. Because more than 30 mg/kg per week of Docetaxel causes body weight loss in mice, 20 mg/kg per week of Docetaxel is judged to be the maximum nontoxic dose. Docetaxel (20 mg/kg per week) is given to mice once a week for 3 weeks at one of the following different points (2, 10, 14, or 22 HALO). Seventy-two hours after the final dosing of the agent, the intestinal mucosa of the small intestine (proximal 8 cm) is removed, fixed in 20 N Mildform solution (containing 8% formaldehyde in a buffered solution), and embedded in paraffin blocks, and sections of 5 μm are put on glass slides. Apoptosis is detected using the terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) method, using the Apop Tag Peroxidase In Situ Apoptosis Detection Kit.
    Rat[4]
    Male Sprague-Dawley rats with body weight between 230-250 g and age between 6-7 weeks are used. About 25 SD rats are divided into five groups receiving Docetaxel (7 mg/kg, i.v.), PIP (35 mg/kg, p.o.) and their combined administration (DOX+PIP) as well as PIP (3.5 mg/kg, p.o.) and PIP (3.5 mg/kg, i.v.). A day before the drug administrations, the rats are anesthetized with an intramuscular injection of a cocktail containing 60 mg/kg ketamine and 6 mg/kg xylazine (injection volume, 0.2 mL). Right jugular vein is cannulated with a polyethylene tubing (0.5 mm ID, 1 mm) for blood collection. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    807.88

    Formula

    C₄₃H₅₃NO₁₄

    CAS No.

    114977-28-5

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 35 mg/mL

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

    Purity: 99.80%

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    Product Name:
    Docetaxel
    Cat. No.:
    HY-B0011
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