生物活性
10058-F4是一种c-Myc抑制剂，特异性抑制c-Myc-Max相互作用，且抑制c-Myc靶基因表达的转录激活。10058-F4抑制白血病细胞生长，且抑制Myc和Max二聚化。10058-F4诱导AML细胞的细胞周期停滞和凋亡。10058-F4使AML细胞停滞在G0/G1期，下调c-Myc的表达，上调CDK抑制剂p21和p27。
化学数据
| 分子量 | 249.35 |
| 分子式 | C12H11NOS2 |
| CAS号 | 403811-55-2 |
| 纯度 | >98.5% |
| 溶解性（25°C） | DMSO 30 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | PC-3 and DU145 cells |
| 方法 | MTT assay
PC-3 cells (2 × 104cells in logarithmic growth) were plated into 96-well culture plates and allowed to adhere to the plates for 24 h prior to the addition of 10058-F4 in medium containing 1% ethanol such that the final concentrations in the wells were 0.1-100 μM in medium containing 0.3% ethanol. After 72 h, 50 μl of 1 mg/ml MTT was added to each well. The cells were washed with medium and phosphate buffered saline, and 150 μl of DMSO was added to each well, followed by shaking for 5 min. The absorbance at 570 nm was read on DYNEX MRX Revelation microplate reader (Dynex, Vienna, VA, USA). Results were compared to wells containing cells treated with vehicle alone and were expressed as % inhibition. The IC50 was calculated using the Hill equation, the program ADAPT II, and data from three separate experiments. |
| 浓度 | 0.1-100 μM |
| 处理时间 | 72 h |
| 动物实验 |
|---|
| 动物模型 | SCID mice bearing DU145 or PC-3 xenografts |
| 配制 | cremophor EL:ethanol:saline (1:1:8 v/v/v) at a final concentration of 2 or 3 mg/ml |
| 剂量 | 20 or 30 mg/kg daily for 5 days for 2 weeks |
| 给药处理 | i.v. |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 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。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.0104 mL | 20.0521 mL | 40.1043 mL |
| 5 mM | 0.8021 mL | 4.0104 mL | 8.0209 mL |
| 10 mM | 0.401 mL | 2.0052 mL | 4.0104 mL |
m.cnreagent.com