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Pixantrone
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。
Pixantrone图片
CAS NO:144675-97-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
马来酸匹衫琼
BBR 2778
产品介绍
Pixantrone (BBR 2778) dimaleate 是一种拓扑异构酶 II (topoisomerase II) 的抑制剂和 DNA 嵌入剂,具有抗肿瘤活性。
生物活性

Pixantrone (BBR 2778) dimaleate is atopoisomeraseIIinhibitor and DNA intercalator, with anti-tumor activity.

IC50& Target[1]

Topoisomerase II

 

体外研究
(In Vitro)

Pixantrone (0-10 μM, 72 h) dimaleate induces cell death in multiple cancer cell lines independent of cell cycle perturbation, with IC50s of 37.3 nM, 126 nM and 136 nM for T47D, MCF-10A and OVCAR5 cells, respectively[1].
Pixantrone (25-500 nM, 2 4 h) dimaleate induces DNA damage at high concentration of 500 nM and induces severe chromosomal aberrations and mitotic catastrophe in PANC1 cells[1].
Pixantrone (100 nM, 24 h) dimaleate may disrupt chromosome segregation because of generating merotelic kinetochore attachments that cause chromosome non-disjunction[1].
Pixantrone (0-100 μM, 72 h) dimaleate potently inhibits growth of human leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK and ABCB1-transfected MDCK/MDR cells with IC50s of 0.10 μM, 0.56 μM, 0.058 μM and 4.5 μM, respectively[2].
Pixantrone (0.01-0.2 μM) dimaleate leads to a concentration-dependent formation of linear DNA through acting on topoisomerase Iiα and produces semiquinone free radicals in an enzymatic reducing system, although not in a cellular system, most likely due to low cellular uptake[2].
Pixantrone (0.01-10 μM) dimaleate shows potent inhibitory activities against rat 97-116 peptide-specific T cell proliferation[4].

体内研究
(In Vivo)

Pixantrone (i.v., 27 mg/kg, every 7 days, three times) dimaleate does not worsen pre-existing moderate degenerative cardiomyopathy, causes minimal cardiotoxic in mice following repeated treatment cycles and results in less mortality than mitoxantrone in doxorubicin-pretreated mice[3].
Pixantrone (i.v., 16.25 mg/kg, every week, three times) dimaleate modulates Lymph node cells (LNC) responses, affacts T cell subpopulations in TAChR-immunized Lewis rats and also shows preventive and therapeutic effect in experimental autoimmune myasthenia gravis (EAMG) rats[4].

Clinical Trial
分子量

557.51

性状

Solid

Formula

C25H27N5O10

CAS 号

144675-97-8

中文名称

马来酸匹衫琼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL(59.78 mM;Need ultrasonic)

H2O : 5 mg/mL(8.97 mM;ultrasonic and warming and heat to 80℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7937 mL8.9684 mL17.9369 mL
5 mM0.3587 mL1.7937 mL3.5874 mL
10 mM0.1794 mL0.8968 mL1.7937 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)。-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: PBS

    Solubility: 50 mg/mL (89.68 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 0.83 mg/mL (1.49 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (1.49 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 8.3 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 0.83 mg/mL (1.49 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (1.49 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。