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96892-57-8

中文名稱 hepsulfam
英文名稱 hepsulfam
CAS 96892-57-8
分子式 C7H18N2O6S2
分子量 290.36
MOL 文件 96892-57-8.mol
96892-57-8 結(jié)構(gòu)式 96892-57-8 結(jié)構(gòu)式

基本信息

中文別名
化合物 T15472
英文別名
hepsulfam
NCI 329680
NSC-329680
ZINC01574758
7-sulfamoyloxyheptyl sulfamate
Sulfamic acid, S,S'-1,7-heptanediyl ester
Bissulfamideoic acid 1,7-heptanediyl ester
Bis(amidosulfuric acid)1,7-heptanediyl ester

物理化學(xué)性質(zhì)

熔點(diǎn)94-95 °C
沸點(diǎn)478.2±55.0 °C(Predicted)
密度1.407±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)9.10±0.70(Predicted)
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
Hepsulfam (NCI 329680; ZINC01574758) 是抗癌試劑,具有優(yōu)異的抗白血病活性,在不同腫瘤中的中位 IC50 值為0.91 μg/mL。
靶點(diǎn)

IC50: 0.91 μg/mL (Tumors)

體外研究

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.

體內(nèi)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.

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