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Docetaxel Trihydrate(RP 56976)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Docetaxel Trihydrate(RP 56976)图片
CAS NO:148408-66-6
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)861.93
FormulaC43H53NO14.3H2O
CAS No.148408-66-6 (Docetaxel Trihydrate);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (116.0 mM)
Water:<1 mg/mL
Ethanol: 100 mg/mL (116.0 mM)
SMILESCC(O[C@@]12CO[C@@H]1C[C@@H]([C@@]3([C@@H]2[C@@H]([C@@]4(C[C@@H](C(C)=C(C4(C)C)[C@H](C3=O)O)OC([C@@H]([C@H](c5ccccc5)NC(OC(C)(C)C)=O)O)=O)O)OC(c6ccccc6)=O)C)O)=O.O.O.O
SynonymsRP56976 (NSC 628503) Trihydrate; RP56976; NSC 628503; RP-56976; NSC628503; RP 56976; NSC-628503; Docetaxel trihydrate, Trade name: Taxotere.
实验参考方法
In Vitro

In vitro activity: 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.


Cell Assay: 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.

In VivoDocetaxel (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.
Animal modelHuman colon carcinomas xenografts CX-1
Formulation & DosageDissolved in 50 mg/mL stock solution in ethanol by adding an equal volume of polysorbate 80 and diluting with 5% dextrose in water to the final volume; 33 mg/kg; i.v. injection
References

Biochem Biophys Res Commun. 1992 Aug 31;187(1):164-70; J Immunol. 1999 Jan 1;162(1):467-73.