Docetaxel

Catalog No.S1148 Batch:S114809

Technical Data

Formula	C₄₃H₅₃NO₁₄
Molecular Weight	807.88	CAS No.	114977-28-5
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (123.78 mM)
		Ethanol	100 mg/mL (123.78 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, 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]

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

: 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]

: Data from [Data independently produced by , , Mol Pharmaceutics, 2014, 11: 2040−50]

Selleck's Docetaxel has been cited by 203 publications

Methylation of GPRC5A promotes liver metastasis and docetaxel resistance through activating mTOR signaling pathway in triple negative breast cancer [ Drug Resist Updat, 2024, 73:101063]	PubMed: 38335844
Cholinergic signaling via muscarinic M1 receptor confers resistance to docetaxel in prostate cancer [ Cell Rep Med, 2024, 5(2):101388]	PubMed: 38262412
Serine/threonine kinase 36 induced epithelial-mesenchymal transition promotes docetaxel resistance in prostate cancer [ Sci Rep, 2024, 14(1):729]	PubMed: 38184689
Nucleolar protein TAAP1/C22orf46 confers pro-survival signaling in non-small cell lung cancer [ Life Sci Alliance, 2024, 7(4)e202302257]	PubMed: 38228372
Targeting prostate tumor low-molecular weight tyrosine phosphatase for oxidation-sensitizing therapy [ Sci Adv, 2024, 10(5):eadg7887]	PubMed: 38295166
Ritonavir reverses resistance to docetaxel and cabazitaxel in prostate cancer cells with acquired resistance to docetaxel [ Cancer Drug Resist, 2024, 7:3]	PubMed: 38318527
Zhoushi Qi Ling decoction inhibits the progression of castration-resistant prostate cancer in vivo by regulating macrophage infiltration via IL6-STAT3 signaling [ J Tradit Complement Med, 2024, 14(1):19-25]	PubMed: 38223804
H3K4me3 remodeling induced acquired resistance through O-GlcNAc transferase [ Drug Resist Updat, 2023, 71:100993]	PubMed: 37639774
High-throughput deconvolution of 3D organoid dynamics at cellular resolution for cancer pharmacology with Cellos [ Nat Commun, 2023, 14(1):8406.]	PubMed: 38114489
Low-dose carboplatin modifies the tumor microenvironment to augment CAR T cell efficacy in human prostate cancer models [ Nat Commun, 2023, 14(1):5346]	PubMed: 37660083

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SHIPPING AND STORAGE
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