2. Cell Cycle/DNA Damage
  3. Topoisomerase
  4. Banoxantrone dihydrochloride

Banoxantrone dihydrochloride  (Synonyms: AQ4N dihydrochloride)

目录号: HY-13562A 纯度: 99.46%
COA 产品使用指南

摩尔计算器

Banoxantrone dihydrochloride 是一种新型生物还原剂，可还原成稳定的 DNA 亲和性化合物 AQ4，AQ4 是一种有效的拓扑异构酶II抑制剂。

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Banoxantrone dihydrochloride Chemical Structure

Banoxantrone dihydrochloride Chemical Structure

CAS No. : 252979-56-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1081
In-stock
1 mg ￥431
In-stock
5 mg ￥950
In-stock
10 mg ￥1650
In-stock
25 mg ￥3700
In-stock
50 mg ￥6000
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Banoxantrone dihydrochloride:

Banoxantrone dihydrochloride 相关抗体

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Topoisomerase Topo I Topo II

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Banoxantrone dihydrochloride is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.

IC50 & Target[1]

Topoisomerase II

 

体外研究
(In Vitro)

Banoxantrone (AQ4N) can be reduced in a hypoxic environment to a stable DNA-affinic agent AQ4. AQ4, a potent topoisomerase II inhibitor, would be capable of damaging cells recruited into the cell cycle following radiation damage to the well-oxygenated cells of the tumor[1]. Banoxantrone shows more than 8-fold higher cytotoxicity under hypoxia than normoxia in cultures of 9L rat gliosarcoma and H460 human non-small-cell lung carcinoma cells but not for 11 other human cancer cell lines. DT-diaphorase protein levels and banoxantrone chemosensitivity are poorly correlated across the cancer cell line panel, and banoxantrone chemosensitivity is not affected by DT-diaphorase inhibitors[2]. Banoxantrone is a bis-N-oxide that is reduced via two sequential two-electron reductions to the tertiary amine, AQ4, which is a potent cytotoxic agent toward both aerobic and hypoxic cells. AQ4, but not AQ4N, intercalates in DNA with high affinity to generate a stable persistent complex that can inhibit topoisomerase II and cause DNA damage and cell death[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Banoxantrone dihydrochloride 相关抗体:
体内研究
(In Vivo)

Banoxantrone (200 mg/kg) significantly enhances the tumor growth delay caused by radiation. This occurred when radiation is administered both as a single dose (12 Gy) and in a multifraction regimen (5x3 Gy). A study of the scheduling of Banoxantrone (AQ4N) administration shows that there is a very long time period over which a maximal effect can be elicited (drug given 4 days before to 6 h after radiation). These results suggest that Banoxantrone has significant potential as a bioreductive drug[1]. The activation of banoxantrone cytotoxicity in vivo requires tumor hypoxia that is more extensive or prolonged than can readily be achieved by vasodilation or by antiangiogenic drug treatment[2]. Incorporation of banoxantrone into conventional chemoradiation protocols therefore targets both oxygenated and hypoxic regions of tumors, and potentially will increase the effectiveness of therapy. A single dose of 60 mg/kg banoxantrone enhances the response of RT112 (bladder) and Calu-6 (lung) xenografts to treatment with cisplatin and radiation therapy. Banoxantrone will increase the efficacy of chemoradiotherapy in preclinical models[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

517.40

Formula

C22H30Cl2N4O6
CAS 号
性状

固体

颜色

Blue to dark blue

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 25 mg/mL (48.32 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H2O 中的溶解度 : 20 mg/mL (38.65 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9327 mL 9.6637 mL 19.3274 mL
5 mM 0.3865 mL 1.9327 mL 3.8655 mL
查看完整储备液配制表

* 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°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

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

    Solubility: ≥ 7.5 mg/mL (14.50 mM); 澄清溶液

    此方案可获得 ≥ 7.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 7.5 mg/mL (14.50 mM); 澄清溶液

    此方案可获得 ≥ 7.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂： PBS

    Solubility: 8.33 mg/mL (16.10 mM); 澄清溶液; 超声助溶 (<60°C)

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.46%

COA (198 KB) HNMR (383 KB) LCMS (99 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[1]

Untreated T50/80 tumors (6.5-9.0 mm geometric diameter (GMD) are excised and gently disaggregated by mechanical disruption in ice-cold phosphate-buffered saline (PBS). Single cell suspensions are prepared by filtration through a 40μm mesh. These are then centrifuged and resuspended in Eagle's minimal essential medium (EMEM) containing 10% fetal calf serum (FCS) at a concentration of 106 cells/mL. Cells (20 mL) are placed in 125 mL rubber sealed glass bottles. These are gassed for 2 h at 37°C to provide welloxygenated conditions, i.e. 95% air/5% carbon dioxide or hypoxic conditions 95% N2/5% CO2. Banoxantrone (AQ4N) (20μM) is added for the last 90 min of this period by injection through the sealed lid. Drug is washed off and cells resuspended in fresh medium. For analysis of DNA damage, aliquots (105 cells) are processed at various times ranging from 0 to 96 h after this procedure. To evaluate the effect of maintaining the excised tumor cells in culture, samples are also maintained in the culture medium above at 37°C, 95% air/5% CO2 for 24 h. The cells, which grow in suspension, are then harvested and placed in glass bottles and the experiment outlined above is carried out. Each experiment is carried out twice and the results pooled[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
T50/80 tumor-bearing mice are used. These experiments are carried out when tumors reach a geometric diameter (GMD) of 6.5-9.0 mm. Banoxantrone (AQ4N) is administered as a single i.p. injection at a dose of 200 mg/kg. The drug is given 30 min before a single dose of X-irradiation of 12 Gy (300 kVp Siemens Stabilipan with a dose rate of 2.56 Gy min-1). Tumors are excised at a range of times following treatment and placed on ice. Single cell suspensions are prepared in ice-cold PBS as outlined above. Following centrifugation the cells are diluted in cold EMEM containing 10% FCS (1x106 cells/mL). An aliquot of 100 μL of this suspension is used in the comet assay. This procedure is carried out on tumors excised at various time intervals ranging from 0 to 120 h following irradiation. The results are pooled from three individual experiments.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Banoxantrone dihydrochloride 相关分类

完整储备液配制表

* 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°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.9327 mL 9.6637 mL 19.3274 mL 48.3185 mL
5 mM 0.3865 mL 1.9327 mL 3.8655 mL 9.6637 mL
10 mM 0.1933 mL 0.9664 mL 1.9327 mL 4.8319 mL
15 mM 0.1288 mL 0.6442 mL 1.2885 mL 3.2212 mL
20 mM 0.0966 mL 0.4832 mL 0.9664 mL 2.4159 mL
25 mM 0.0773 mL 0.3865 mL 0.7731 mL 1.9327 mL
30 mM 0.0644 mL 0.3221 mL 0.6442 mL 1.6106 mL
DMSO 40 mM 0.0483 mL 0.2416 mL 0.4832 mL 1.2080 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Banoxantrone252979-56-9AQ4NTopoisomeraseInhibitorinhibitorinhibit

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