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Docetaxel

Catalog No. T1034 CAS 114977-28-5

Synonyms: NSC 628503, RP-56976

Docetaxel (RP-56976) is a semi-synthetic analog of paclitaxel, a microtubule depolymerization inhibitor (IC50=0.2 μM). Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression and exhibits apoptosis-inducing, anti-tumor activity.

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Docetaxel, CAS 114977-28-5

Pack Size	Availability	Price/USD
25 mg	In stock	$ 30.00
50 mg	In stock	$ 39.00
100 mg	In stock	$ 57.00
200 mg	In stock	$ 82.00
500 mg	In stock	$ 136.00
1 g	In stock	$ 197.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.29%

Purity: 99.15%

Purity: 99.03%

Purity: 98.92%

Biological Description

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Storage & Solubility Information

Description	Docetaxel (RP-56976) is a semi-synthetic analog of paclitaxel, a microtubule depolymerization inhibitor (IC50=0.2 μM). Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression and exhibits apoptosis-inducing, anti-tumor activity.
Targets&IC50	Microtubule:0.2 μM
In vitro	METHODS: Human lung cancer cells NCI-H460 were treated with Docetaxel (0.2-200 nmol/L) for 24-72 h, and cell viability was measured by MTS. RESULTS: The IC50 of NCI-H460 to Docetaxel was 0.030 μmol/L at 72 h and 0.116 μmol/L at 24 h. [1] METHODS: Human prostate cancer cells PC-3, DU-145 and LNCaP were treated with Docetaxel (0.5-4 nM) for 48 h. Apoptosis was detected by Flow Cytometry. RESULTS: High-dose Docetaxel treatment significantly increased the proportion of Annexin V+ apoptotic cells. [2]
In vivo	METHODS: To detect anti-tumor activity in vivo, Docetaxel (5-10 mg/kg) and PD-1 inhibitor (200 μg/only) were intraperitoneally injected into CB17 SCID mice carrying mouse prostate cancer tumor RM-1 five times a week for ten days. RESULTS: PD-1 inhibitor combined with Docetaxel had a synergistic effect on prostate cancer in mice, inhibiting the growth of prostate tumors, increasing the survival rate and reducing adverse effects. [3] METHODS: To assay antitumor activity in vivo, Docetaxel (7.5-15 mg/kg, intratumorally injected IT twice weekly for six weeks; or 20-40 mg/kg weekly intravenously injected IV) was administered to C57BL/6 mice harboring HNSCC tumors HN30 or HN12. RESULTS: IT Docetaxel improved overall survival and disease-free survival and reversed tumor growth. At equivalent dose levels, IT Docetaxel resulted in 26-fold higher peak tumor concentrations and 24-fold longer tumor exposure than IV treatment. [4]
Cell Research	NCI-H460 cells (4 × 10^3) were grown in 100 μl of DMEM medium containing serum per well in a 96-well plate. After 24 h, the cells were treated with docetaxel (0, 0.2, 0.63, 2, 6.3, 20, 63 and 200 nmol/L, respectively) for 72 h. Every treatment was triplicate in the same experiment. Then 20 μl of MTS was added to each well for 1 to 4 h at 37°C. After incubation, the absorbance was read at a wavelength of 490 nm according to the manufacturer's protocol. The IC50 calculation was performed with GraphPad Prism 5.0 software [2].
Animal Research	Docetaxel (0, 10, 20, 30, 40, 60, and 80 mg/kg per week) was given once a week for 3 weeks for mice. Because more than 30 mg/kg per week of the drug caused body weight loss in mice, 20 mg/kg per week of docetaxel was judged to be the maximum nontoxic dose. Docetaxel (20 mg/kg per week) was given to mice once a week for 3 weeks at one of the following different points (2, 10, 14, or 22 HALO). Seventy-two hours after the final dosing of the agent, the intestinal mucosa of the small intestine (proximal 8 cm) was removed, fixed in 20 N Mildform solution (containing 8% formaldehyde in a buffered solution), and embedded in paraffin blocks, and sections of 5 mm were put on glass slides. Apoptosis was detected using the terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) method, using the Apop Tag Peroxidase In Situ Apoptosis Detection Kit. Specimens were dewaxed and immersed in phosphate-buffered saline for 5 minutes at room temperature, incubated with 20 mg/ml proteinase K for 15 minutes at room temperature, and then quenched of endogenous peroxidase in 2% hydrogen peroxide in phosphate-buffered saline. Terminal deoxynucleotidyl transferase enzyme was applied directly onto the specimens, which were then incubated at 37°C for 1 hour. The reaction was terminated by transferring the slides to stop/wash buffer for 10 minutes at room temperature, and then specimens were covered with peroxidase-conjugated anti-digoxigenin antibody and incubated for 30 minutes at room temperature. Specimens were then soaked in staining buffer containing 0.05% diaminobenzidine to achieve color development. Finally, the specimens were counterstained by immersion in Mayer's hematoxylin solution. Apoptotic cells were counted under a light microscope in a good longitudinal crypt section. Starting at the base of the crypt column, the TUNEL-positive cells were counted up to the 18th cell position in each crypt.One hundred crypt sections were scored in each animal, and a frequency of TUNELpositive cells per crypt was calculated. Dosing time-dependent influence of docetaxel on intestinal apoptosis was also examined in female Balb/c mice [5].
Source	Natural Products > Caryophyllaceae > Dianthus

Synonyms	NSC 628503, RP-56976
Molecular Weight	807.88
Formula	C43H53NO14
CAS No.	114977-28-5

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 80.8 mg/mL (100 mM)

DMSO: 80.8 mg/mL (100 mM)

References and Literature

1. Che CL, et al. DNA microarray reveals different pathways responding to paclitaxel and docetaxel in non-small cell lung cancer cell line. Int J Clin Exp Pathol. 2013 Jul 15;6(8):1538-48. 2. Yang C, et al. Effect of docetaxel on the regulation of proliferation and apoptosis of human prostate cancer cells. Mol Med Rep. 2019 May;19(5):3864-3870. 3. Zhou S, et al. PD-1 inhibitor combined with Docetaxel exerts synergistic anti-prostate cancer effect in mice by down-regulating the expression of PI3K/AKT/NFKB-P65/PD-L1 signaling pathway. Cancer Biomark. 2024 Jan 17. 4. Yoo GH, et al. An in vivo evaluation of docetaxel delivered intratumorally in head and neck squamous cell carcinoma. Arch Otolaryngol Head Neck Surg. 2005 May;131(5):418-29. 5. Obi-Ioka Y, et al. Involvement of Wee1 in the circadian rhythm dependent intestinal damage induced by docetaxel. J Pharmacol Exp Ther. 2013 Oct;347(1):242-8. 6. Attia RT, et al. The chemomodulatory effects of glufosfamide on docetaxel cytotoxicity in prostate cancer cells. PeerJ. 2016 Jun 29;4:e2168. 7. Li C, et al. Non-linear pharmacokinetics of piperine and its herb-drug interactions with docetaxel in Sprague-Dawley rats. J Pharm Biomed Anal. 2016 Sep 5;128:286-93. 8. Chen Y, Li K, Gong D, et al. ACLY: A biomarker of recurrence in breast cancer. Pathology-Research and Practice. 2020: 153076. 9. Dong H, Sun H, Zheng J. A microchip for integrated single-cell genotoxicity assay[J]. Talanta. 2016, 161: 804-811. 10. Li Q, Qin T, Bi Z, et al. Rac1 activates non-oxidative pentose phosphate pathway to induce chemoresistance of breast cancer[J]. Nature Communications. 2020, 11(1): 1-18.

Citations

1. Li Q, Qin T, Bi Z, et al. Rac1 activates non-oxidative pentose phosphate pathway to induce chemoresistance of breast cancer. Nature Communications. 2020, 11(1): 1-18. 2. Chen Y, Li K, Gong D I, et al. ACLY: A biomarker of recurrence in breast cancer. Pathology-Research and Practice. 2020, 216(9): 153076 3. Wavelet-Vermuse C, Odnokoz O, Xue Y, et al. CDC20-Mediated hnRNPU Ubiquitination Regulates Chromatin Condensation and Anti-Cancer Drug Response. Cancers. 2022, 14(15): 3732. 4. Dong H, Sun H, Zheng J. A microchip for integrated single-cell genotoxicity assay. Talanta. 2016, 161: 804-811. 5. Liu S, Tao Y, Wu S, et al.Sanguinarine chloride induces ferroptosis by regulating ROS/BACH1/HMOX1 signaling pathway in prostate cancer.Chinese Medicine.2024, 19(1): 1-18. 6. Tao Y, Lu J, Li L, et al.Raltitrexed induces apoptosis through activating ROS-mediated ER stress by impeding HSPA8 expression in prostate cancer cells.Biochimica et Biophysica Acta (BBA)-Molecular Cell Research.2024: 119684.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Microtubule-Targeted Compound Library Anti-Cancer Active Compound Library EMA Approved Drug Library Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Apoptosis Compound Library Anti-Tumor Natural Product Library

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Keywords

Docetaxel 114977-28-5 Apoptosis Cytoskeletal Signaling Metabolism Microtubule Associated Endogenous Metabolite NSC628503 inhibit Inhibitor NSC 628503 RP 56976 RP56976 NSC-628503 RP-56976 Microtubule/Tubulin inhibitor

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