Docetaxel |
| رقم الكتالوجGC16684 |
دوسيتاكسيل هو دواء مضاد للأورام يعمل عن طريق تثبيط تحلل الأنابيب الدقيقة والتخفيف من آثار تعبير جينات bcl-2 و bcl-xL.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 114977-28-5
Sample solution is provided at 25 µL, 10mM.
Docetaxel is a taxane class of anti-mitotic chemotherapeutic agents with an IC50 of 0.2 µM. It preferentially binds to β-tubulin, suppresses microtubule dynamics, disrupts cell division, and therefore effectively induces apoptosis. Docetaxel has anti-cancer activity[1-3].
Docetaxel(5 uM;24-72h) suppressed PC-3M IE8 cell proliferation and aerobic glycolysis[4]. Docetaxel(50 nM; 12-48 h) inhibited the proliferation while it enhanced the apoptosis of human CD133 expressing HCC stem cells[5]. Docetaxel treatment activates lysosomal function and promotes its fusion with autophagosome[6].
Docetaxel-based(10 mg/kg Docetaxel per injection；i.p; once per week for two consecutive weeks) chemohormonal therapy prompted the intratumoral infiltration of T cells and upregulated the abundance of PD1 and PD-L1, thereby sensitizing mouse tumors to the anti-PD1 blockade in a xenograft mouse model[7-8].
References:
[1]. James ND, Sydes MR, et,al. Addition of docetaxel, zoledronic acid, or both to first-line long-term hormone therapy in prostate cancer (STAMPEDE): survival results from an adaptive, multiarm, multistage, platform randomised controlled trial. Lancet. 2016 Mar 19;387(10024):1163-77. doi: 10.1016/S0140-6736(15)01037-5. Epub 2015 Dec 21. PMID: 26719232; PMCID: PMC4800035.
[2]. Sweeney CJ, Chen YH, et,al. Chemohormonal Therapy in Metastatic Hormone-Sensitive Prostate Cancer. N Engl J Med. 2015 Aug 20;373(8):737-46. doi: 10.1056/NEJMoa1503747. Epub 2015 Aug 5. PMID: 26244877; PMCID: PMC4562797.
[3]. Buey RM, DÍaz JF, et,al. Interaction of epothilone analogs with the paclitaxel binding site: relationship between binding affinity, microtubule stabilization, and cytotoxicity. Chem Biol. 2004 Feb;11(2):225-36. doi: 10.1016/j.chembiol.2004.01.014. PMID: 15123284.
[4]. Peng J, He Z, et,al. Docetaxel suppressed cell proliferation through Smad3/HIF-1α-mediated glycolysis in prostate cancer cells. Cell Commun Signal. 2022 Dec 19;20(1):194. doi: 10.1186/s12964-022-00950-z. PMID: 36536346; PMCID: PMC9762006.
[5]. Zhang X, Shao J, et,al. Docetaxel promotes cell apoptosis and decreases SOX2 expression in CD133‑expressing hepatocellular carcinoma stem cells by suppressing the PI3K/AKT signaling pathway. Oncol Rep. 2019 Feb;41(2):1067-1074. doi: 10.3892/or.2018.6891. Epub 2018 Nov 27. PMID: 30483804.
[6]. Zhang J, Wang J, et,al. Docetaxel enhances lysosomal function through TFEB activation. Cell Death Dis. 2018 May 23;9(6):614. doi: 10.1038/s41419-018-0571-4. PMID: 29795139; PMCID: PMC5966422.
[7]. Ma Z, Zhang W, et,al. Docetaxel remodels prostate cancer immune microenvironment and enhances checkpoint inhibitor-based immunotherapy. Theranostics. 2022 Jun 27;12(11):4965-4979. doi: 10.7150/thno.73152. PMID: 35836810; PMCID: PMC9274752.
[8]. Yu Y, Yang FH, et,al. Mesenchymal stem cells desensitize castration-resistant prostate cancer to docetaxel chemotherapy via inducing TGF-beta1-mediated cell autophagy. Cell Biosci. 2021;11(1):7.
| Cell experiment [1]: | |
|
Cell lines |
PC-3M IE8 cells |
|
Preparation Method |
PC-3M IE8 cells were digested and reseeded in a 96-well plate, and treated with Docetaxel. The cell viability of cells was determined by CCK-8 assay. |
|
Reaction Conditions |
5 uM; 24-72h |
|
Applications |
Docetaxel suppressed cell proliferation. |
| Animal experiment [2]: | |
|
Animal models |
5 weeks old male C57BL/6J mice (Subcutaneous anti-castrated prostate cancer mouse model) |
|
Preparation Method |
Mice were inoculated with RM1 cells, and on day 7, mice carrying RM1 cells were castrated bilaterally under anesthesia. When the subcutaneous tumor volume reached the standard, the mice were randomly divided into 4 groups, which were respectively given intrabitoneal administration (DMSO, anti-PD1, bicalutamide and docetaxel), and the tumor volume was measured every 3 days. |
|
Dosage form |
10 mg/kg Docetaxel per injection；i.p; once per week for two consecutive weeks |
|
Applications |
Docetaxel inhibits tumor development. |
|
References: [1]. Peng J, He Z, et,al. Docetaxel suppressed cell proliferation through Smad3/HIF-1α-mediated glycolysis in prostate cancer cells. Cell Commun Signal. 2022 Dec 19;20(1):194. doi: 10.1186/s12964-022-00950-z. PMID: 36536346; PMCID: PMC9762006. |
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| Cas No. | 114977-28-5 | SDF | |
| Canonical SMILES | O=C(N[C@H]([C@H](C(O[C@H]1C[C@]2(O)C(C)(C)C([C@@H](O)C([C@@]3(C)[C@]([C@@](CO4)(OC(C)=O)[C@@]4([H])C[C@@H]3O)([H])[C@@H]2OC(C5=CC=CC=C5)=O)=O)=C1C)=O)O)C6=CC=CC=C6)OC(C)(C)C | ||
| Formula | C43H53NO14 | M.Wt | 807.88 |
| الذوبان | ≥ 40.4mg/mL in DMSO, ≥ 94.4 mg/mL in EtOH | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.2378 mL | 6.189 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 |
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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