Docetaxel

製品コードS1148 バッチS114811

印刷

化学情報

Chemical Structure Synonyms NSC 628503,RP56976 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C43H53NO14
分子量 807.88 CAS No. 114977-28-5
Solubility (25°C)* 体外 DMSO 100 mg/mL (123.78 mM)
Ethanol 100 mg/mL (123.78 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 30%PEG300 5%Tween80 60%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.000mg/ml (2.48mM) Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 600 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.
in vitro Docetaxel is a cytotoxic agent, especially for proliferating cells, which is related to its ability to promote the formation of microtubule bundles and induce sustained mitotic arrest, followed by apoptosis of mitotically arrested cells or permanent mitotic block. This compound suppresses microtubule dynamic instability as well as tread-milling, resulting in the failure of chromosomes to segregate to the daughter cells, which in turn triggers premature exit from mitosis rather than a block at this phase of the cell cycle. [2] It inhibits the clonogenic survival of Human cancer cell Hs746T (stomach), AGS (stomach), HeLa (cervix), CaSki (cervix), BxPC3 (pancreas), Capan-1 (pancreas) with IC50 of 1 nM, 1 nM, 0.3 nM, 0.3 nM, 0.3 nM and 0.3 nM respectively. [4] This agent inhibits endothelial cell migration that does not affects microtubule gross morphology or inhibit cell proliferation, although they does produce more subtle effects on microtubule dynamics. It inhibits HUVEC migration with an observed IC50 of 1 pM. HUVEC chemotaxis stimulated by either of two angiogenic factors, thymidine phosphorylase or VEGF, is inhibited by this chemical with IC 50 of 10 pM and is ablated at 1 nM. [7] It induces human monocytes, but not RAW 264.7 murine macrophages, Prostaglandin H Synthase-2m (PGHS-2) expression. [8]
in vivo Docetaxel (33 mg/kg/dose, given i.v. every 4 days for 3 injections) results in a tumor growth delay of 19.3 days in M2OL2 colon xenografts. This compound also shows great antitumor activities in MX-1, SK-MEL-2, LX-1 and OVCAR-3 xenografts. It inhibits the angiogenic response to fibroblast growth factor 2 with IC 50 of 5.4 mg/kg when injected twice weekly over a 14-day period, and angiogenesis is completely blocked in mice that receives 10 mg/kg of this chemical. It has selectivity for endothelial cell migration and/or microvessel formation because infiltration of inflammatory cells into the Matrigel plug is much less sensitive to inhibition by this compound. [7]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human gastric cancer cell lines MKN-28
濃度 6 nM
反応時間 3 days
実験の流れ 2000 cells in 180 μL of medium are seeded in a 96-well plate, and 20 μL of drug solution is simultaneously added in triplicate to each well. The plate is incubated for 3 days at 37°C in a humidified atmosphere of 5% CO2. On day 3, 25 μL of MTT reagent is added to each well. After 4 h of incubation, the medium is removed by aspiration. 0.2 mL of dimethylsulphoxide (DMSO) is added to each well and thoroughly mixed by using a mechanical plate mixer to dissolve the resulting MTT-formazan crystals. Absorbance at 540 nm (OD) is measured by a reader.
動物実験 動物モデル Human colon carcinomas xenografts CX-1
投薬量 33 mg/kg
投与方法 i.v. every 4 days for 3 injections

参考

  • https://pubmed.ncbi.nlm.nih.gov/15123284/
  • https://pubmed.ncbi.nlm.nih.gov/1381586/
  • https://pubmed.ncbi.nlm.nih.gov/16899972/
  • https://pubmed.ncbi.nlm.nih.gov/7906583/
  • https://pubmed.ncbi.nlm.nih.gov/8664032/
  • https://pubmed.ncbi.nlm.nih.gov/12479700/
  • https://pubmed.ncbi.nlm.nih.gov/9886421/
  • https://pubmed.ncbi.nlm.nih.gov/7499102/

カスタマーフィードバック

Data from [Data independently produced by J Transl Med, 2013, 0.6]

Data from [Data independently produced by J Transl Med, 2013, 0.6]

Data from [Data independently produced by , , Cell, 2018, 174(5):1200-1215]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Off-pore nucleoporin sPOM121 transcriptionally propels β-Catenin driven tumor progression and immune escape in prostate cancer [ Cancer Discov, 2025, 10.1158/2159-8290.CD-25-0629] PubMed: 40709833
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Pristimerin Promotes Ubiquitination of HSPA8 and Activates the VAV1/ERK Pathway to Suppress TNBC Proliferation [ Adv Sci (Weinh), 2025, 12(10):e2413174] PubMed: 39813169
Prediction of Patient Drug Response via 3D Bioprinted Gastric Cancer Model Utilized Patient-Derived Tissue Laden Tissue-Specific Bioink [ Adv Sci (Weinh), 2025, 12(10):e2411769] PubMed: 39748450
Organoid morphology-guided classification for oral cancer reveals prognosis [ Cell Rep Med, 2025, 6(5):102129] PubMed: 40359934
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MUC1-C dependence in treatment-resistant prostate cancer uncovers a target for antibody-drug conjugate therapy [ JCI Insight, 2025, 10(14)e190924] PubMed: 40553569
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Mechanism of Action and Interaction of Garlic Extract and Established Therapeutics in Prostate Cancer [ Int J Mol Sci, 2025, 26(4)1777] PubMed: 40004239
Targeting YY1-DR5 Axis by Pyripyropene O as a Novel Therapeutic Strategy Against Prostate Cancer: Molecular Mechanisms and In Vivo Zebrafish Validation [ Mar Drugs, 2025, 23(5)214] PubMed: 40422804

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人間や獣医の診断であるか治療的な使用のためにでない。

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