IZCZ-3 是有效的c-MYC转录抑制剂，具有抗肿瘤活性。
| 生物活性 | IZCZ-3 is a potentc-MYCtranscriptioninhibitor with antitumor activity[1]. |
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体外研究
(In Vitro) | IZCZ-3 (2.1 μM-15.9 μM; 24 hours) significantly inhibits SiHa, HeLa, Huh7, and A375 cancer cell proliferation (IC50s of 3.3, 2.1，4.1, and 4.2 μM, respectively). IZCZ-3 induces only weak growth inhibition in the BJ fibroblasts (IC50=15.9 μM) and mouse mesangial cells (IC50=15.6 μM), suggesting that IZCZ-3 is more effective against cancer cells than against c-MYC-independent normal cells[1].
IZCZ-3 (0-5 μM; 12 hours) induces an apparent accumulation of cells in the G0/G1 phase in SiHa cells in a dose-dependent manner[1].
Cell Proliferation Assay[1] | Cell Line: | SiHa, HeLa, Huh7, and A375 cancer cells (with overexpression of c-MYC protein) and in normal BJ fibroblasts and primary cultured mouse mesangial cells (with relatively low expression of c-MYC protein). | | Concentration: | 2.1 μM-15.9 μM | | Incubation Time: | 24 hours | | Result: | IC50s of 3.3, 2.1，4.1, and 4.2 μM for SiHa, HeLa, Huh7, and A375 cancer cells; IC50s of 15.9 μM and 15.6 μM for BJ fibroblasts and mouse mesangial cells. |
Cell Cycle Analysis[1] | Cell Line: | SiHa cells | | Concentration: | 0, 1.25, 2.5, and 5 μM | | Incubation Time: | 12 hours | | Result: | Induced an apparent accumulation of cells in the G0/G1 phase (increasing from 61% to 70%) in a dose-dependent manner. |
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体内研究
(In Vivo) | IZCZ-3 (20, 10, and 5 mg/kg; intraperitoneally; every other day for 24 days) inhibits tumor growth in BALB/c nude mice with SiHa human cervical squamous cancer xenograft[1].
| Animal Model: | BALB/c nude mice (5 weeks old) bearing SiHa human cervical squamous cancer xenograft model[1] | | Dosage: | 20, 10, and 5 mg/kg | | Administration: | Treated intraperitoneally; every other day for 24 days | | Result: | Treatment with 20, 10, and 5 mg/kg resulted in a significant reduction in tumor weight with tumor growth inhibition (TGI) of 69%, 64%, and 57%, respectively. Displayed time-dependent inhibition of tumor growth. |
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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 : 5 mg/mL(6.98 mM;ultrasonic and warming and heat to 80℃) 配制储备液 | 1 mM | 1.3968 mL | 6.9839 mL | 13.9678 mL | | 5 mM | 0.2794 mL | 1.3968 mL | 2.7936 mL | | 10 mM | --- | --- | --- |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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