LQZ-7I 是一种靶向survivin的抑制剂。LQZ-7I 抑制生存素二聚化。LQZ-7I 口服有效抑制异种移植肿瘤生长并诱导肿瘤中生存素的损失。
生物活性 | LQZ-7I is asurvivin-targeting inhibitor. LQZ-7I inhibitssurvivindimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and inducessurvivinloss in tumors[1]. |
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体外研究 (In Vitro) | LQZ-7I has improved cytotoxicity with IC50s of 3.1 μM against C4-2 cells and 4.8 μM against PC-3 cells compared with the parent compound LQZ-7[1]. LQZ-7I (10 μM; 0-6 hours) treatment reduces the expression of survivin. However, LQZ-7I does not reduce the expression of XIAP, CIAP1, and CIAP2. LQZ-7I may be selective to its intended target survivin[1].
Western Blot Analysis[1] Cell Line: | PC-3 or C4-2 cells | Concentration: | 10 μM | Incubation Time: | 0-6 hours | Result: | Reduced the expression of survivin. |
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体内研究 (In Vivo) | LQZ-7I (100 mg/kg; oral gavage every other day for a total of ten treatments) significantly suppresses tumor growth without any notable adverse effect on the mice[1].
Animal Model: | 6-week old male NSG mice[1] | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 125 mg/mL(358.83 mM;Need ultrasonic) 配制储备液 1 mM | 2.8707 mL | 14.3534 mL | 28.7068 mL | 5 mM | 0.5741 mL | 2.8707 mL | 5.7414 mL | 10 mM | 0.2871 mL | 1.4353 mL | 2.8707 mL |
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