Docetaxel (RP56976)

Catalog No.S1148 Synonyms: NSC 628503

For research use only.

Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

Docetaxel (RP56976) Chemical Structure

CAS No. 114977-28-5

Selleck's Docetaxel (RP56976) has been cited by 137 publications

Purity & Quality Control

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Biological Activity

Description Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.
Targets
Microtubules [1]
(Cell-free assay)
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. Docetaxel 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] Docetaxel 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] Docetaxel 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. Docetaxel 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 Docetaxel with IC 50 of 10 pM and is ablated at 1 nM. [7] Docetaxel induces human monocytes, but not RAW 264.7 murine macrophages, Prostaglandin H Synthase-2m (PGHS-2) expression. [8]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HSC-3 NGr1SmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDSO4pLUUN3ME2wMlAxODF|MjFOwG0> NGHsRnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6Oi9pPmPBUmdGWjxxYU6=
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NCI-H292 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnlVFZKSzVyPUCuNFAxOTV7IN88US=> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5Nk8oRlODTlfFVlww[T5?
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Assay
Methods Test Index PMID
Western blot PIM1 ; cyclin B ; pSTAT3 / STAT3 ; p-p53 / p53 18426800 22996738
Immunofluorescence α-tubulin ; cleaved PARP / cleaved caspase-3 ; Acetylated tubulin ; SQSTM1 / LAMP1 27177833 21087597 18426800 29795139
Growth inhibition assay Cell viability 22996738
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. Docetaxel also shows great antitumor activities in MX-1, SK-MEL-2, LX-1 and OVCAR-3 xenografts. Docetaxel 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 Docetaxel. Docetaxel 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 Docetaxel. [7]

Protocol (from reference)

Cell Research:[5]
  • Cell lines: Human gastric cancer cell lines MKN-28
  • Concentrations: 6 nM
  • Incubation Time: 3 days
  • Method: 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.
  • (Only for Reference)
Animal Research:[6]
  • Animal Models: Human colon carcinomas xenografts CX-1
  • Dosages: 33 mg/kg
  • Administration: i.v. every 4 days for 3 injections
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(123.78 mM)
Water Insoluble
Ethanol '53 mg/mL warmed

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

2mg/mL

* 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.

Chemical Information

Molecular Weight 807.88
Formula

C43H53NO14

CAS No. 114977-28-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C2C(C(=O)C3(C(CC4C(C3C(C(C2(C)C)(CC1OC(=O)C(C(C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)O)C)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05027204 Not yet recruiting Drug: Docetaxel|Drug: Nivolumab Squamous Cell Carcinoma of Head and Neck CSPC ZhongQi Pharmaceutical Technology Co. Ltd. September 2021 Phase 1|Phase 2
NCT04467801 Recruiting Drug: Ipatasertib NSCLC Stage IV|NSCLC Stage IIIB Jun Zhang MD PhD|University of Iowa|University of Kentucky|University of Kansas Medical Center August 18 2021 Phase 2
NCT04811118 Recruiting Drug: Docetaxel for Injection (Albumin-bound)|Drug: Taxotere Advanced Solid Tumors CSPC ZhongQi Pharmaceutical Technology Co. Ltd. May 18 2021 Phase 1
NCT04823910 Not yet recruiting -- Prostate Cancer Physiomics|Portsmouth Hospitals NHS Trust|National Institute for Health Research United Kingdom May 2021 --
NCT04889599 Recruiting Drug: BH009 (Docetaxel injection)|Drug: Docetaxel injection Docetaxel|Solid Tumours|Bioequivalence Zhuhai Beihai Biotech Co. Ltd April 29 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2021-09-06)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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