hepsulfam
- CAS号:96892-57-8
- 英文名:hepsulfam
- 中文名:hepsulfam
- CBNumber:CB41378537
- 分子式:C7H18N2O6S2
- 分子量:290.36
- MOL File:96892-57-8.mol
- 熔点 :94-95 °C
- 沸点 :478.2±55.0 °C(Predicted)
- 密度 :1.407±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 形态 :Solid
- 酸度系数(pKa) :9.10±0.70(Predicted)
- 颜色 :White to off-white
hepsulfam性质、用途与生产工艺
- 生物活性 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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靶点
IC50: 0.91 μg/mL (Tumors)
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体外研究
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. 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.
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体内研究
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.
- 更新日期:2024/08/19
- 产品编号:HY-U00095
- 产品名称:hepsulfam Hepsulfam
- CAS编号:96892-57-8
- 包装:1mg
- 价格:720元
- 更新日期:2024/08/19
- 产品编号:HY-U00095
- 产品名称:hepsulfam Hepsulfam
- CAS编号:96892-57-8
- 包装:5mg
- 价格:1440元
- 公司名称:MedChemexpress LLC
- 联系电话:021-58955995
- 电子邮件:sales@medchemexpress.cn
- 国家:美国
- 产品数:4863
- 优势度:58
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:19892
- 优势度:58
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58