F14512 is a polyamine-containing inhibitor of DNA topoisomerase II with a broad spectrum of antitumor activities.
别名：F-14512
F14512 is a polyamine-containing inhibitor of DNA topoisomerase II with a broad spectrum of antitumor activities. In P388 leukemia cells, activation of the DNA damage response by F14512 did not induce immediate apoptosis but resulted in an early growth arrest. F14512-induced G2 arrest was accompanied by the appearance of a senescence-like phenotype (characterized by an increased β-galactosidase staining) with up-regulation of the cyclin-dependent kinase inhibitor p16, and cyclin D1. The early senescence-based cell cycle block was characterized by a marked increase of the level of the IAP protein survivin, but not cIAP2, in P388 cells as well as in three other leukemia and melanoma cell types.
F14512 significantly inhibited tumor growth compared to etoposide, in a cisplatin-resistant A2780R subcutaneous model, at a dose of 1.25 mg/kg.
| 分子量 | 641.76 |
| 分子式 | C33H47N5O8 |
| CAS号 | 866874-63-7 |
| 储存条件 |
粉末型式 -20°C 3年；4°C 2年 溶于溶剂 -80°C 6个月；-20°C 1个月 |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.5582 mL | 7.7911 mL | 15.5821 mL |
| 5 mM | 0.3116 mL | 1.5582 mL | 3.1164 mL |
| 10 mM | 0.1558 mL | 0.7791 mL | 1.5582 mL |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
| 其他相关的Topoisomerase产品 |
|---|
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Topoisomerase II inhibitor 13 是一种拓扑异构酶 II (Topo II) 抑制剂。 |
| ICRF-196
ICRF-196 是 ICRF-193 的 (S,S)- 和 (R,R)- 异构体的外消旋混合物。 |
| Cholesteryl hemisuccinate
Cholesteryl hemisuccinate 是一种具有保肝和抗癌活性的物质。 |
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