165668-41-7
中文名称
N-(3-氯-1H-吲哚-7-基)-1,4-苯二磺酰胺
英文名称
Indisulam
CAS
165668-41-7
分子式
C14H12ClN3O4S2
分子量
385.85
MOL 文件
165668-41-7.mol
更新日期
2025/01/09 18:04:24
165668-41-7 结构式
基本信息
中文别名
化合物INDISULAMN-(3-氯-1H-吲哚-7-基)-1,4-苯二磺酰胺
英文别名
D04522E-7070
ER-35744
INDISULAM
IndisulaM (E7070)
E7070
ER-35744
D04522
Indisulam >=98% (HPLC)
IndisulaM (E7070) (ER-35744)
N-(3-Chloro-1H-indol-7-yl)-1,4-benzenedisulfonamide
N1-(3-Chloro-1H-indol-7-yl)benzene-1,4-disulfonamide
所属类别
生物化工：激动剂抑制剂物理化学性质
熔点242-243 °C (decomp)(Solv: ethanol (64-17-5); water (7732-18-5))
沸点668.9±65.0 °C(Predicted)
密度1.663±0.06 g/cm3(Predicted)
储存条件-20°C
溶解度DMSO : 100 mg/mL (259.17 mM; Need ultrasonic)
酸度系数(pKa)8.14±0.30(Predicted)
形态粉末
颜色白色至米色
常见问题列表
生物活性
Indisulam (E7070) 是一种有效的 carbonic anhydrase (CA) 抑制剂，可抑制 cytosolic isozymes I 和 II 以及与肿瘤相关的跨膜 isozyme IX。Indisulam 可抑制 cyclin E 的表达和 CDK2 的磷酸化，这两者对于G1期到S期的转变都是必不可少的。靶点
| Target | Value |
|
CA
() | |
|
cyclin E
() | |
|
CDK2
() |
体外研究
Indisulam (E7070, 0-50 μg/mL, 12-48 h) causes cell cycle perturbation in the G1 phase in a time- and dose-dependent manner, potentially leading to cell death.
Cell Cycle Analysis
| Cell Line: | P388 murine leukaemia cells. |
| Concentration: | 0-50 μg/mL. |
| Incubation Time: | 12-48 h. |
| Result: | Accumulated P388 cells in the G1 phase. |
体内研究
Indisulam (E7070, 12.5, 25, 50 (100) mg/kg) shows an antitumour spectrum in human cancer models.
| Animal Model: | Female BALB/c nu/nu mice aged 7 weeks (HCT116 colon, LX-1 lung, SW620 colon, HCT115 colon, PC-9 lung, DLD-1 colon and WiDr colon models). |
| Dosage: | 12.5, 25, 50 (100) mg/kg. |
| Administration: | IV daily for 4 days. |
| Result: | Exhibited anti-tumor activity. |