Home Cytoskeletal Signaling Microtubule Associated inhibitor Docetaxel Trihydrate For research use only.

Docetaxel Trihydrate

Synonyms: RP56976 (NSC 628503) Trihydrate

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

Docetaxel Trihydrate Chemical Structure

Docetaxel Trihydrate Chemical Structure

CAS No. 148408-66-6

Purity & Quality Control

Batch: S778701 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.96%
99.96

Docetaxel Trihydrate Related Products

Signaling Pathway

Microtubule Associated Signaling Pathways

Microtubule Associated Signaling Pathway

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]
In vitro
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 Research 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.
In Vivo
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]
Animal Research Animal Models Human colon carcinomas xenografts CX-1
Dosages 33 mg/kg
Administration i.v. every 4 days for 3 injections
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06319313 Not yet recruiting
Squamous Cell Non-small Cell Lung Cancer
Shanghai JMT-Bio Inc.
 May 1 2024 Phase 2|Phase 3
NCT06200558 Not yet recruiting
Prostate Cancer
Hospital of Macerata
 January 31 2024 --
NCT05156372 Withdrawn
Prostate Cancer Metastatic|Castrate Resistant Prostate Cancer|Metastatic Prostate Cancer|Metastatic Prostate Adenocarcinoma
The University of Texas Health Science Center at San Antonio
 December 2023 Not Applicable

Chemical Information & Solubility

Molecular Weight 861.93 Formula

C43H53NO14.3H2O
CAS No. 148408-66-6 SDF Download Docetaxel Trihydrate SDF
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.O.O.O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (116.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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