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Hepsulfam

Hepsulfam

产品编号 T15472   CAS 96892-57-8
别名: NCI 329680, ZINC01574758

Hepsulfam is an anticancer agent. It also displays excellent antileukemic activity (a median IC50: 0.91 μg/mL in a panel of different tumors).

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Hepsulfam Chemical Structure
Hepsulfam, CAS 96892-57-8
规格 价格/CNY 货期 数量
2 mg ¥ 1,210 5日内发货
25 mg ¥ 6,760 6-8周
50 mg ¥ 8,790 6-8周
100 mg ¥ 13,600 6-8周
1 mL * 10 mM (in DMSO) ¥ 2,650 5日内发货
产品目录号及名称: Hepsulfam (T15472)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Hepsulfam is an anticancer agent. It also displays excellent antileukemic activity (a median IC50: 0.91 μg/mL in a panel of different tumors).
靶点活性 Tumors:0.91 μg/ml
体外活性 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 causes a higher level of DNA interstrand cross-links than busulfan. Hepsulfam (1.0 μg/mL) 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 shows a higher activity of hepsulfam, especially in non-small cell lung cancer[1]. 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].
体内活性 The preclinical activity of hepsulfam shows a possible role of this compound in the treatment of solid human malignancies. Hepsulfam demonstrates superior in vivo activity in a large cell lung cancer xenograft and a gastric carcinoma model. The increased bone marrow toxicity of hepsulfam as compared with the busulfan might be critical for further clinical application[1].
别名 NCI 329680, ZINC01574758
分子量 290.36
分子式 C7H18N2O6S2
CAS No. 96892-57-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Berger DP, et al. Preclinical activity of hepsulfam and busulfan in solid human tumor xenografts and human bone marrow. Anticancer Drugs. 1992 Oct;3(5):531-9. 2. Pacheco DY, et al. Mechanisms of toxicity of hepsulfam in human tumor cell lines. Cancer Res. 1990 Dec 1;50(23):7555-8.

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Hepsulfam 96892-57-8 Others NCI 329680 ZINC-01574758 ZINC01574758 ZINC 01574758 NCI329680 NCI-329680 Inhibitor inhibitor inhibit

 

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