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生物活性
10058-F4 blocks the C-MYC/Max heterodimerization which is required for c-Myc activity as a transcription factor. 10058-F4 efficiently inhibits the induction of PGC-1β mRNA by both HRG and IGF-1 and also abolishes the induction of PGC-1β protein levels by HRG and IGF-1, confirming that the induction of PGC-1b protein by these growth factors is a transcriptional event requiring C-MYC activity.[2] 10058-F4 acts not only to block c-Myc function through the mechanism of c-Myc/Max heterodimer dissociation, but it also resulted in decreased c-Myc mRNA levels (65%, n = 3) in lymphoma cells.
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体外研究
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体内研究
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激酶实验
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细胞实验
0, 30, 60, 90, 120, 150 μM
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动物实验
20 或 30 mg/kg 静脉注射
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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）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
[1] Huang MJ, et al. Exp Hematol, 2006, 34(11), 1480-1489.
[2] Lin, C.P., et al. 2007. Anticancer Drugs. 18: 161-170.
[3] Guo, J., et al. 2009. Cancer Chemother. Pharmacol. 63: 615-625.
分子式
C12H11NOS2 |
分子量
249.35 |
CAS号
403811-55-2 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
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DMSO
100 mM |
Water
<1 mg/mL |
Ethanol
20 mM |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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