Docetaxel Trihydrate

Catalog No.S7787 Batch:S778701

Technical Data

Formula	C₄₃H₅₃NO₁₄.3H₂O
Molecular Weight	861.93	CAS No.	148408-66-6
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (116.01 mM)
		Ethanol	100 mg/mL (116.01 mM)
		Water	Insoluble
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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]

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]

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 Assay:^{^[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.
Animal Study:^{^[6]}	Animal Models Human colon carcinomas xenografts CX-1 Dosages 33 mg/kg Administration i.v. every 4 days for 3 injections

Cell Assay:^{^[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.

Animal Study:^{^[6]}

Animal Models
Human colon carcinomas xenografts CX-1
Dosages
33 mg/kg
Administration
i.v. every 4 days for 3 injections

References

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Customer Product Validation

: , , Mol Pharm, 2014, 11(7):2040-50.

: , , J Transl Med, 2013, 11:204.

: , , PLoS One,2015, 10(4):e0123901

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

Selleck's Docetaxel Trihydrate has been cited by 66 publications

Combating castration-resistant prostate cancer by co-targeting the epigenetic regulators EZH2 and HDAC [ PLoS Biol, 2023, 21(4):e3002038]	PubMed: 37104245
MARCKSL1-2 reverses docetaxel-resistance of lung adenocarcinoma cells by recruiting SUZ12 to suppress HDAC1 and elevate miR-200b [ Mol Cancer, 2022, 21(1):150]	PubMed: 35864549
Docetaxel remodels prostate cancer immune microenvironment and enhances checkpoint inhibitor-based immunotherapy [ Theranostics, 2022, 12(11):4965-4979]	PubMed: 35836810
Therapeutic targeting of glutamate dehydrogenase 1 that links metabolic reprogramming and Snail-mediated epithelial-mesenchymal transition in drug-resistant lung cancer [ Pharmacol Res, 2022, 185:106490]	PubMed: 36216131
The therapeutic effect of KSP inhibitors in preclinical models of cholangiocarcinoma [ Cell Death Dis, 2022, 13-9:799]	PubMed: 36123339
Toll-Like Receptor 3 Overexpression Induces Invasion of Prostate Cancer Cells, whereas Its Activation Triggers Apoptosis [ Am J Pathol, 2022, S0002-9440(22)00174-2]	PubMed: 35750257
Establishment and large-scale validation of a three-dimensional tumor model on an array chip for anticancer drug evaluation [ Front Pharmacol, 2022, 13:1032975]	PubMed: 36313330
Imidazo[4,5-b]pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis [ Bioorg Chem, 2022, 127:106032]	PubMed: 35872398
Betacellulin promotes tumor development and EGFR mutant lung cancer growth by stimulating the EGFR pathway and suppressing apoptosis [ Bioengineered, 2022, 13(4):11310-11320]	PubMed: 35499128
Gene therapy of prostate cancer using liposomes containing perforin expression vector driven by the promoter of prostate-specific antigen gene [ Sci Rep, 2022, 12(1):1442]	PubMed: 35087064

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SHIPPING AND STORAGE
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