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Pirarubicin Hydrochloride
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。
Pirarubicin Hydrochloride图片
CAS NO:95343-20-7

盐酸吡柔比星
THP Hydrochloride
Pirarubicin Hydrochloride (THP Hydrochloride) 是一种蒽环类抗生素,为拓扑异构酶 II (topoisomerase II) 的抑制剂,可用于各种癌症尤其是实体瘤的研究。
生物活性

Pirarubicin Hydrochloride is an anthracyclineantibiotics, acts as atopoisomeraseIIinhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.

IC50& Target[1]

Topoisomerase II

 

体外研究
(In Vitro)

Pirarubicin is a topoisomerase II inhibitor[1]. Pirarubicin shows inhibitory activities against M5076 and Ehrlich cells, with IC50s of 0.366 and 0.078 μM, respectively. The cytotoxicity of Pirarubicin toward M5076 cells is lower than toward Ehrlich cells, and this is due to the much lower expression of topoisomerase II in M5076 cells than in Ehrlich cells[2]. Pirarubicin (2.5, 5, 10 μg/mL) significantly induces autophagy in a dose dependent manner in bladder cancer (T24, EJ, 5637, J82 and UM-UC-3) cells. Furthmore, Pirarubicin (5 μg/mL) induces apoptosis through inhibition of mTOR/p70S6K/4E-BP1 in bladder cancer cells, and this effect is enhanced by inhibition of autophagy[3].

体内研究
(In Vivo)

Pirarubicin (18 mg/kg, i.v.) significantly elevates serum level of BNP, CK-MB, CTnT, LDH, and MDA compared with those in the control group in acute cardiac toxicity rats. Pirarubicin also lowers heart rate, and depresses R-wave voltage, and prolongation of QT intervals in the acute cardiac toxicity model[4].

Clinical Trial
分子量

664.10

性状

Solid

Formula

C32H38ClNO12

CAS 号

95343-20-7

中文名称

盐酸吡柔比星;盐酸吡喃阿霉素;盐酸吡柔吡星

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 20.83 mg/mL(31.37 mM;Need ultrasonic)

H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.5058 mL7.5290 mL15.0580 mL
5 mM0.3012 mL1.5058 mL3.0116 mL
10 mM0.1506 mL0.7529 mL1.5058 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (3.13 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.13 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。
 
 
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