Docetaxel
(Synonyms: 多西他赛; RP-56976) 目录号 : GC16684
Docetaxel是紫杉烷类抗有丝分裂化疗药物,IC50为0.2 µM。
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.
Docetaxel是紫杉烷类抗有丝分裂化疗药物,IC50为0.2 µM。它优先与β-微管蛋白结合,抑制微管动力学,破坏细胞分裂,从而有效诱导细胞凋亡。Docetaxel具有抗癌活性[1-3]。
Docetaxel(5 uM;24-72h)抑制PC-3M IE8细胞增殖和有氧糖酵解[4]。Docetaxel(50 nM; 12-48 h)抑制细胞增殖,同时促进表达CD133的人HCC干细胞的凋亡[5]。Docetaxel治疗激活溶酶体功能,促进其与自噬体融合[6]。
Docetaxel(10 mg/kg Docetaxel per injection；i.p; once per week for two consecutive weeks) 为基础的化学激素治疗促进肿瘤内T细胞浸润,上调PD1和PD-L1的丰度,从而使小鼠肿瘤对抗PD1阻断物敏感[7-8]。
| Cell experiment [1]: | |
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Cell lines |
PC-3M IE8 cells |
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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. |
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Reaction Conditions |
5 uM; 24-72h |
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Applications |
Docetaxel suppressed cell proliferation. |
| Animal experiment [2]: | |
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Animal models |
5 weeks old male C57BL/6J mice (Subcutaneous anti-castrated prostate cancer mouse model) |
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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. |
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Dosage form |
10 mg/kg Docetaxel per injection；i.p; once per week for two consecutive weeks |
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Applications |
Docetaxel inhibits tumor development. |
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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 | |
| 别名 | 多西他赛; RP-56976 | ||
| 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 | ||
| 分子式 | C43H53NO14 | 分子量 | 807.88 |
| 溶解度 | ≥ 40.4mg/mL in DMSO, ≥ 94.4 mg/mL in EtOH | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet