Docetaxel Trihydrate|148408-66-6|-陌孚医药/Medlife

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Docetaxel Trihydrate

目录号: PL07228 纯度: ≥99%

CAS No. :148408-66-6

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中文名称	Docetaxel Trihydrate
中文别名	三水多烯紫杉醇;多西他赛三水合物;多西他赛;多西他赛(三水);多西他赛Docetaxel;多西紫杉醇;多烯紫杉醇;多烯紫杉醇(三水);多烯紫杉醇三水合物;多烯紫杉醇三水合物标准品;多烯紫杉醇系统适应性 EP标准品;三水多西他赛;三水多西紫杉醇 EP标准品;三水多烯紫杉醇 USP标准品;三水盐酸伊立替康;三水多西;多西他赛三水物;多西他赛三水化合物;多似紫杉醇(三水);多烯紫杉醇(三水合物);多烯紫杉醇三水(标准品);多西他赛 , 多烯紫杉醇(三水合物)
英文名称	Docetaxel Trihydrate
英文别名	docetaxel trihydrate;Docetaxel·Trihydrate;Docetaxel;Docetaxel (Trihydrate);DOCETAXEL HYDRATE;Unii-15H5577cqd;Xrp6976;Benzenepropanoicacid, b-[[(1,1-dimethylethoxy)carbonyl]amino]-a-hydroxy-,(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-ylester, trihydrate, (aR,bS)- (9CI);Benzenepropanoic acid, b-[[(1,1-dimethylethoxy)carbonyl]amino]-a-hydroxy-,12b-(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-ylester trihydrate, [2aR-[2aa,4b,4ab,6b,9a(aR,bS),11a,12a,12aa,12ba]]-;7,11-Methano-1H-cyclodeca[3,4]benz[1,2-b]oxete,benzenepropanoic acid deriv.;Docetaxel (200 mg);Taxotere Trihydrate;Docetaxel(trihydrous);RP56976 (NSC 628503) Trihydrate;(2AR,4S,4aS,6R,9S,11S,12S,12aS,12bS)-12b-acetoxy-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-;7,11-Methano-1H-cyclodeca[3,4]benz[1,2-b]oxete, benzenepropanoic acid deriv.;[(1S,2S,3R,7R,9S,10S,12R,15S)-4-Acetyloxy-1,9,12-trihydroxy-15-[(2R,3S)-2-hydroxy-3-[(2-methylpropan;[(1S,2S,3R,7R,9S,10S,12R,15S)-4-Acetyloxy-1,9,12-trihydroxy-15-[(2R,3S)-2-hydroxy-3-[(2-methylpropan-2-yl)oxycarbonylamino]-3-phenylpropanoyl]oxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl] benzoate;trihydrate;15H5577CQD;Taxotere (TN);Docetaxel Trihydrate
Cas No.	148408-66-6
分子式	C₄₃H₅₉NO₁₇
分子量	861.93
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Docetaxel Trihydrate (RP-56976 Trihydrate) 是一种抗肿瘤试剂,抑制微管解聚 (microtubule depolymerization) 的 IC₅₀ 值为 0.2 μM。Docetaxel Trihydrate 是紫杉醇的半合成类似物，能减弱 bcl-2 和 bcl-xL 基因表达的影响。Docetaxel Trihydrate 阻滞G2/M细胞周期，导致细胞凋亡 (apoptosis)。

生物活性

Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC 50 value of 0.2 μM. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis.

性状

Solid

IC50 & Target[1][2]

Microtubule

体外研究(In Vitro)

Docetaxel Trihydrate (RP-56976 Trihydrate) and Glufosfamide (GLU) single and combined treatments affect the cells viability in a dose-dependent manner. The IC50 of GLU are 70±4 μM and 86.8±8 μM in PC-3 and LNCaP cells; respectively. While, the IC50 of Docetaxel alone is found to be 3.08±0.4 nM and 1.46±0.2 nM in PC-3 and LNCaP cells; respectively. The co-treatment of GLU with Docetaxel is found to synergize the cytotoxicity and the IC50 values are decreased to be 2.7±0.1 nM and 0.75±0.3 nM in PC-3 and LNCaP cells; respectively. IC50 of NCI-H460 to Docetaxel at 24 h is 116 nM and at 72 h is 30 nM. According to data reported in DTP Data Search, the mean IC50 of NCI-60 cell panel to Docetaxel is 14-34 nM. has not independently confirmed the accuracy of these methods. T

体内研究(In Vivo)

In female mice, the Docetaxel Trihydrate (RP-56976 Trihydrate)-induced intestinal apoptosis in the 14-hours after light on (HALO) group is significantly greater than that in the 2-HALO group. Bax expression is significantly elevated by Docetaxel in the 2-HALO group, but not in the 14-HALO group. On the other hand, cleaved Caspase-3 expression is significantly elevated by Docetaxel in the 14-HALO group, but not in the 2-HALO group. The expressions of Wee1 and phosphorylated CKD1 are significantly elevated after dosing of Docetaxel at 14 HALO, but not at 2 HALO. In addition, Docetaxel significantly reduces survivin expression in the 14-HALO group but not in the 2-HALO group. The survivin expression level in the Docetaxel-treated 14-HALO group is significantly smaller than that in the drug-treated 2-HALO group. Piperine (PIP) is administrated via intravenous bolus at 3.5 mg/kg an

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Attia RT, et al. The chemomodulatory effects of glufosfamide on docetaxel cytotoxicity in prostate cancer cells. PeerJ. 2016 Jun 29;4:e2168.
[2]. 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.

溶解度数据	In Vitro: DMSO : 250 mg/mL (290.05 mM; Need ultrasonic)Ethanol : 50 mg/mL (58.01 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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