受注:045-509-1970 |
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Synonyms | RP56976 (NSC 628503) Trihydrate | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C43H53NO14.3H2O |
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分子量 | 861.93 | CAS No. | 148408-66-6 | |
Solubility (25°C)* | 体外 | 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. |
製品説明 | Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules. |
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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] |
細胞アッセイ | 細胞株 | Human gastric cancer cell lines MKN-28 |
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濃度 | 6 nM | |
反応時間 | 3 days | |
実験の流れ | 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. | |
動物実験 | 動物モデル | Human colon carcinomas xenografts CX-1 |
投薬量 | 33 mg/kg | |
投与方法 | i.v. every 4 days for 3 injections |
, , Mol Pharm, 2014, 11(7):2040-50.
, , J Transl Med, 2013, 11:204.
, , PLoS One,2015, 10(4):e0123901
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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