For research use only.
Catalog No.S7787 Synonyms: RP56976 (NSC 628503) Trihydrate
CAS No. 148408-66-6
Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.
Selleck's Docetaxel Trihydrate has been cited by 30 publications
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Choose Selective Microtubule Associated Inhibitors
|Description||Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.|
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.  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.  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.  Docetaxel induces human monocytes, but not RAW 264.7 murine macrophages, Prostaglandin H Synthase-2m (PGHS-2) expression. 
|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. |
-  Buey RM. Chem Biol, 2004, 11(2), 225-236.
-  Riou JF, et al. Biochem Biophys Res Commun, 1992, 187(1), 164-170.
-  Balcer-Kubiczek EK, et al. Chemotherapy, 2006, 52(5), 231-240.
|In vitro||DMSO||100 mg/mL (116.01 mM)|
|Ethanol||100 mg/mL (116.01 mM)|
* 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.
|Synonyms||RP56976 (NSC 628503) Trihydrate|
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04656652||Not yet recruiting||Drug: DS-1062a|Drug: Docetaxel||Non-small Cell Lung Cancer||Daiichi Sankyo Inc.|AstraZeneca||December 14 2020||Phase 3|
|NCT04471675||Recruiting||Drug: Albumin-bound docetaxel||Advanced Solid Tumors||CSPC ZhongQi Pharmaceutical Technology Co. Ltd.||December 2 2020||Phase 1|
|NCT04396535||Recruiting||Drug: Bintrafusp Alfa|Drug: Docetaxel||Advanced Lung Non-Small Cell Carcinoma|Stage III Lung Cancer AJCC v8|Stage IIIA Lung Cancer AJCC v8|Stage IIIB Lung Cancer AJCC v8|Stage IIIC Lung Cancer AJCC v8|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8||Mayo Clinic|National Cancer Institute (NCI)||October 23 2020||Phase 2|
|NCT04533958||Recruiting||Device: HYPNO VR® device||Metastatic Prostate Cancer||Saint-Gregoire Private Hospital Center||September 28 2020||Not Applicable|
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.
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