产品
编 号:F243892
分子式:C20H14F2N4
分子量:348.35
产品类型
结构图
CAS No: 195822-23-2
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产品详情
生物活性:
LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors.
体内研究:
LQZ-7I (100 mg/kg;隔日灌胃,共 10 次处理) 显著抑制肿瘤生长,对小鼠没有任何明显的不良影响。Animal Model:6-week old male NSG mice
Dosage:100 mg/kg; 200 μL vehicle (90% corn oil/10% DMSO)
Administration:Oral gavage every other day for a total of ten treatments
Result:Significantly suppressed tumor growth without any notable adverse effect on the mice as indicated by lacking changes in body weight and in wet weight of major organs at the end of the study.
体外研究:
与母体化合物 LQZ-7 相比,LQZ-7I 提高了细胞毒性,对 C4-2 细胞的 IC50 为 3.1 μM,对 PC-3 细胞的 IC50 为 4.8 μM。 LQZ-7I (10 μM;0-6 小时) 处理可降低生存素的表达。然而,LQZ-7I 不会降低 XIAP、CIAP1 和 CIAP2 的表达。LQZ-7I 可能对其预期目标 survivin 具有选择性。