Docetaxel Trihydrate

产品说明书

Print
Chemical Structure| 148408-66-6 同义名 : 多西他赛三水合物 ;RP-56976 Trihydrate
CAS号 : 148408-66-6
货号 : A335487
分子式 : C43H59NO17
纯度 : 98%
分子量 : 861.93
MDL号 : MFCD26960948
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(290.05 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 50 mg/mL(58.01 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
生物活性
描述 Microtubules are the main constituent of mitotic apparatus in all eukaryotic cells, thus make it become an important pharmacological target for the treatment of tumor . Docetaxel Trihydrate is the trihydrate form of Docetaxel. Docetaxel, belong to the taxane family including paclitaxel, can promote the assembly and polymerization of microtubule with an appearance of twice as active in depolymerization inhibition compared with paclitaxel . When treated with Docetaxel for 72h, the significant growth inhibition can be observed in ovarian cancer cell line, including A2780, H134, IGROV-1 and OVCAR-3, with IC50 ranging from 2.8-87nM. Activation of caspase, upregulation of Bcl-2 phosphorylation and apoptosis can be observed in cells with prolonged G2/M arrest by Docetaxel, which may be one of the mechanism for cell death induced by Docetaxel in tumor therapy. However, Docetaxel also shows antiangiogenic effect in in vitro and in vivo studies. It can inhibit HUVEC proliferation in a dose-dependent manner with an IC50 of 0.27 ng/ml, as well as reduce 54% of angiogenesis level compared with control on dose of 3 mg/kg in MCF-7 tumor bearing nude mice .Docetaxel is approved by FDA for treatment of head and neck cancer, gastric cancer, breast cancer, prostate cancer and non-small cell lung cancer (see in FDA net).
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.16mL

0.23mL

0.12mL

5.80mL

1.16mL

0.58mL

11.60mL

2.32mL

1.16mL
参考文献

[1]Buey RM, Diaz JF, et al. Interaction of epothilone analogs with the paclitaxel binding site: relationship between binding affinity, microtubule stabilization, and cytotoxicity. Chem Biol. 2004 Feb;11(2):225-36.

[2]Riou JF, Naudin A, Lavelle F. Effects of Taxotere on murine and human tumor cell lines. Biochem Biophys Res Commun. 1992 Aug 31;187(1):164-70.