1. Cell Cycle/DNA Damage
    Apoptosis
    Cytoskeleton
  2. Microtubule/Tubulin
    Apoptosis
  3. Docetaxel

Docetaxel (Synonyms: RP-56976)

製品番号: HY-B0011 純度: 99.96%
取扱説明書

Docetaxel (RP-56976) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM. Docetaxel (RP-56976) is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel (RP-56976) arrests the cell cycle at G2/M and leads to cell apoptosis.

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Docetaxel 構造式

Docetaxel 構造式

CAS 番号 : 114977-28-5

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 79 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 72 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 102 在庫あり
Estimated Time of Arrival: December 31
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 11 publication(s) in Google Scholar

Other Forms of Docetaxel:

Top Publications Citing Use of Products

    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.
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    製品説明

    Docetaxel (RP-56976) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM. Docetaxel (RP-56976) is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel (RP-56976) arrests the cell cycle at G2/M and leads to cell apoptosis.

    IC50 & Target

    Microtubule[1]

    体外実験

    Docetaxel (RP-56976) 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].

    体内実験

    In female mice, the Docetaxel (RP-56976)-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].

    臨床実験
    分子量

    807.88

    分子式

    C₄₃H₅₃NO₁₄

    CAS 番号

    114977-28-5

    SMILES

    O=C(OC(C)(C)C)N[[email protected]@H](C1=CC=CC=C1)[[email protected]](C(O[[email protected]@H]2C(C)=C([[email protected]@H](O)C([[email protected]@]3(C)[[email protected]]([[email protected]@](CO4)(OC(C)=O)[[email protected]@]4([H])C[[email protected]@H]3O)([H])[[email protected]@H]5OC(C6=CC=CC=C6)=O)=O)C(C)(C)[[email protected]@]5(O)C2)=O)O

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 35 mg/mL (43.32 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.09 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (3.09 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.09 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    細胞実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [3][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.
    Rats[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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 99.96%

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    Keywords:

    DocetaxelRP-56976RP56976RP 56976Microtubule/TubulinApoptosisInhibitorinhibitorinhibit

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    製品名:
    Docetaxel
    製品番号:
    HY-B0011
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