2. Cell Cycle/DNA Damage Apoptosis
  3. Topoisomerase Apoptosis
  4. Voreloxin Hydrochloride

Voreloxin Hydrochloride  (Synonyms: SNS-595 Hydrochloride; Vosaroxin Hydrochloride; AG 7352 Hydrochloride)

目录号: HY-16518 纯度: 99.96%
COA 产品使用指南

摩尔计算器

Voreloxin Hydrochloride 是一种新创的拓扑异构酶 II (topoisomerase II) 抑制剂，能够诱导 DNA 双链断裂，阻滞 G2 期，最终细胞凋亡。

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Voreloxin Hydrochloride Chemical Structure

Voreloxin Hydrochloride Chemical Structure

CAS No. : 175519-16-1

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100 mg ￥6800
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Customer Review

Other Forms of Voreloxin Hydrochloride:

Voreloxin Hydrochloride 相关抗体

Top Publications Citing Use of Products

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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

Voreloxin Hydrochloride is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.

IC50 & Target

Topoisomerase II

 

体外研究
(In Vitro)

Voreloxin Hydrochloride is a first-in-class topoisomerase II poison and inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis. Voreloxin (0.1-20 µM) inhibits topoisomerase II activity and induces site-selective DNA DSB in CCRF-CEM cells. Voreloxin (0.11, 0.33, 1, 3 µM) induces G2 arrest partially through topoisomerase II in A549 lung cancer cell line. Voreloxin cytotoxic activity requires DNA intercalation. However, Voreloxin (1-9 µM) does not generate significant levels of ROS[1]. Voreloxin has potent cytotoxic activity in AML cell lines MV4-11 and HL-60, with IC50s of 95 ± 8 nM and 884 ± 114 nM, respectively. Voreloxin in combination with cytarabine shows additive or synergistic activity in acute leukemia cell lines[2]. Voreloxin is active on the primary acute myeloid leukemia (AML) with a mean LD50 of 2.3 μM. The LD50 for voreloxin in myeloid cell lines NB4 and HL-60 is 0.59 μM ± 0.25 μM. Voreloxin causes accumulation of cells in the S and G2 phases of the cell cycle and acts on topoisomerase II[3].

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

Voreloxin Hydrochloride 相关抗体:
体内研究
(In Vivo)

Voreloxin (20 mg/kg, i.v.) alone results in 80% reduction in bone marrow cellularity of CD-1 mice by administration one dose every 4 days repeated twice (q4d ×2). voreloxin at 10 mg/kg in combination with cytarabine causes ablation of the marrow, dilation of sinusoids, and infiltration of adipocytes in mice. Voreloxin (20 mg/kg, i.v.) combined with cytarabine causes a reversible decrease in myeloid and lymphoid cells in bone marrow and peripheral blood CD-1 mice. voreloxin (10 mg/kg, q4d ×2) and cytarabine in combination causes reversible neutropenia with a more modest impact on platelets CD-1 mice[2].

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

437.90

Formula

C18H20ClN5O4S
CAS 号
性状

固体

颜色

White to gray

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: 

H2O 中的溶解度 : 2 mg/mL (4.57 mM; 超声助溶 (<60°C))

DMSO 中的溶解度 : 2 mg/mL (4.57 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2836 mL 11.4181 mL 22.8363 mL
5 mM --- --- ---
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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 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

In Vivo:

以下溶解方案，请直接配置工作液。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: 2 mg/mL (4.57 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
纯度 & 产品资料

纯度: 99.96%

COA (267 KB) LCMS (120 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[3]

In vitro toxicity assays are performed on primary AML mononuclear cells over a 48 h period using a MTS cell proliferation assay. Lethal doses (LD50) are calculated. Cells are treated with voreloxin (31.25 nM to 4 μM) and Ara-C (62.5 nM to 8 μM) by serial dilution and incubated for 48 h in a final volume of 90 μL. Following the incubation, 20 μL of MTS reagent are added and the reaction is incubated for a further 4 h. The absorbance of the reaction after this time is read by spectrophotometry at 490 nm and the percentage of viable cells calculated relative to untreated control cells in the same assay. IC50 values are calculated using Calcusyn software[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Animals are weighed, randomized by body weight, and assigned to the study groups before initiation of treatment. Voreloxin is administered intravenously (IV) at 10 or 20 mg/kg once on day zero and once on day four (q4d ×2). Cytarabine is administered subcutaneously (SC) at 20 or 60 mg/kg every 8 h on day zero and day four (tid q4d ×2). Tissues and blood are sampled on days 6, 8, and 12 from at least three and not greater than ten animals per treatment group. Femurs are placed in Streck Tissue Fixative solution, or in 10% formalin solution for 24-48 h followed by a 70% dehydrant (ethanol, isopropanol, methanol). Femurs are decalcified, paraffin embedded, and sectioned at Biopathology Labs. The four micron sections are stained with hematoxylin-eosin (H&E). H&E stained femurs are examined and percent cellularity of the bone marrow is determined. Digital photographs of representative femur sections are taken on a Leica DM2000 microscope using Image-Pro Plus v6.1 software[2].

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

Voreloxin Hydrochloride 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.2836 mL 11.4181 mL 22.8363 mL 57.0907 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:

Voreloxin175519-16-1SNS-595VosaroxinAG 7352SNS595SNS 595AG7352AG-7352TopoisomeraseApoptosisInhibitorinhibitorinhibit

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