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Hepsulfam  (Synonyms: NCI 329680; ZINC01574758)

目录号: HY-U00095 纯度: 99.31%
COA 产品使用指南

Hepsulfam (NCI 329680; ZINC01574758) 是抗癌试剂,具有优异的抗白血病活性,在不同肿瘤中的中位 IC50 值为0.91 μg/mL。

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Hepsulfam Chemical Structure

Hepsulfam Chemical Structure

CAS No. : 96892-57-8

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10 mM * 1 mL in DMSO ¥2300
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1 mg ¥720
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5 mg ¥1440
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10 mg ¥2448
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20 mg ¥3900
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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.

IC50 & Target

IC50: 0.91 μg/mL (Tumors)[1]

体外研究
(In Vitro)

At a concentration of 1.0 μg/mL, hepsulfam is active in eight of 37 tumors (22%) in the clonogenic assay. Hepsulfam demonstrates a clear in vitro toxicity to human bone marrow cells (CFU-GM) from healthy donors. Evaluation of equitoxic concentrations in vitro reveals a higher activity of hepsulfam, especially in non-small cell lung cancer[1]. Hepsulfam is more toxic to L1210 leukemia cells than is busulfan, its structural homologue . Consistent with the difference in toxicity, hepsulfam induces DNA interstrand cross-links in L1210 mouse leukemia cells, whereas busulfan does not. Hepsulfam is more cytotoxic to two human leukemia cell lines (111-60 and K562) and to two human colon carcinoma cell lines (BE and HT-29) than is busulfan. As in 11210 cells, hepsulfam induces a higher level of DNA interstrand cross-links than busulfan. Hepsulfam is also more cytotoxic to the human leukemia cell lines when the concentrations are reduced 10-fold and the duration of drug exposure is increased to 12 h[2].

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

体内研究
(In Vivo)

Hepsulfam demonstrates superior in vivo activity in a large cell lung cancer xenograft and a gastric carcinoma model. The preclinical activity of hepsulfam suggests a possible role of this compound in the treatment of solid human malignancies. However, the increased bone marrow toxicity of hepsulfam as compared with busulfan might be critical for further clinical application[1].

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

分子量

290.36

Formula

C7H18N2O6S2

CAS 号
性状

固体

颜色

White to off-white

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (344.40 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)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4440 mL 17.2200 mL 34.4400 mL
5 mM 0.6888 mL 3.4440 mL 6.8880 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, 6 months; -20°C, 1 month。-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。

  • 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

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: 99.31%

参考文献
Cell Assay
[2]

HL-60 or K562 leukemia cells (1x106/mL) are treated with various concentrations of hepsulfam for 2, 3,6, 9, or 12 h at 37°C. The concentration of DMSO in either control or treated cells is never greater than 2% (v/v). Following drug exposure, the cells are ished by centrifugation in RPMI 1640 medium and resuspended in fresh medium. Following this ish, cells are either assayed immediately for DNA damage by alkaline elution or incubated at 37°C for various periods before assay. BE and HT-29 human colon carcinoma cells are processed for alkaline elution analysis or cytotoxicity assays[2].

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

参考文献

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。-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
DMSO 1 mM 3.4440 mL 17.2200 mL 34.4400 mL 86.1000 mL
5 mM 0.6888 mL 3.4440 mL 6.8880 mL 17.2200 mL
10 mM 0.3444 mL 1.7220 mL 3.4440 mL 8.6100 mL
15 mM 0.2296 mL 1.1480 mL 2.2960 mL 5.7400 mL
20 mM 0.1722 mL 0.8610 mL 1.7220 mL 4.3050 mL
25 mM 0.1378 mL 0.6888 mL 1.3776 mL 3.4440 mL
30 mM 0.1148 mL 0.5740 mL 1.1480 mL 2.8700 mL
40 mM 0.0861 mL 0.4305 mL 0.8610 mL 2.1525 mL
50 mM 0.0689 mL 0.3444 mL 0.6888 mL 1.7220 mL
60 mM 0.0574 mL 0.2870 mL 0.5740 mL 1.4350 mL
80 mM 0.0431 mL 0.2153 mL 0.4305 mL 1.0763 mL
100 mM 0.0344 mL 0.1722 mL 0.3444 mL 0.8610 mL
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.

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