LMP744 (MJ-III65) 是一种 DNA 嵌合剂，是拓扑异构酶 1 (Top1)抑制剂，具有抗肿瘤活性。
| 生物活性 | LMP744 (MJ-III65) is a DNA intercalator andTopoisomeraseI (Top1)inhibitor with antitumor activity[1]. |
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体外研究
(In Vitro) | The GI50value of LMP744 (MJ-III-65) for NCI60 cells is 0.1 μM[2].
LMP744 (0.1-5 μM, 3 days) induces dose-dependent accumulation of cells in the S and G2phases of the cell cycle[2].
Cell Viability Assay[2] | Cell Line: | P388 and P388 Top1-deficient murine leukemia cells | | Concentration: | 0.1-100 μM | | Incubation Time: | 3 days | | Result: | Induced dose-dependent accumulation of cells in the S and G2phases of the cell cycle. |
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体内研究
(In Vivo) | LMP744 (MJ-III65) (10-50 mg/kg) administered i.v. push once a week for 4 weeks in nude mice moderately actives against human A253 and FaDu tumor xenografts without significant toxicity[1].
| Animal Model: | Athymic nude mice (nu/nu, female, 20-25 g, 8-12 weeks old) transplanted with A253 and FaDu human head and neck xenografts[1]. | | Dosage: | 10, 25, or 50 mg/kg/week, 4 weeks | | Administration: | I.V. push via tail vein | | Result: | Moderately actived against human A253 and FaDu tumor xenografts without significant toxicity. |
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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 : ≥ 4.17 mg/mL(9.22 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.2101 mL | 11.0507 mL | 22.1014 mL | | 5 mM | 0.4420 mL | 2.2101 mL | 4.4203 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。 |
