产品
编 号:F276734
分子式:C9H8N4O5
分子量:252.18
产品类型
结构图
CAS No: 21919-05-1
联系客服
产品详情
生物活性:
Tretazicar (CB 1954), an antitumor proagent, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1).
体内研究:
Tretazicar (CB 1954) (80 mg/kg;腹腔注射,第 2 天和第 9 天) 可显著提高存活率。Animal Model:Female BALB/c mice (AB22-nr, SKOV3 human ovarian tumour xenograft)
Dosage:80 mg/kg
Administration:i.p. on days 2 and 9
Result:The median survival of the AB22-nr was 49 days. Resulted in a significant increase in survival.
体外研究:
Tretazicar (CB 1954) (0.1-1000 μM;3 天) 对逆转录病毒转导的 AB22 (AB22-nr) 细胞具有敏感性,IC50 为 3 μM。 受影响细胞中 DNA 交联的形成是 Walker 细胞中 DT 心肌黄酶 (NAD (P) H 脱氢酶 (醌)) 对药物进行生物活化的结果,该酶可减少 4-硝基 Tretazicar 组。该反应的产物是双官能团烷化剂 5-aziridin-1-yl-4-hydroxylamino-2-nitrobenzamide。