生物活性

Pifithrin-α is firstly found to block the activation of p53-responsive lacZ in ConA cells and reduce activation of endogenous cellular p53-responsive genes. In MEF cells transformed with E1a+ras, 10μM Pifithrin-α can inhibit the apoptosis of the cells and this anti-apoptotic activity is p53-dependent. Pifithrin-α also inhibits the growth arrest of human diploid fibroblasts induced by DNA damage but has no effect on p53-deficient fibroblasts. In addition, Pifithrin-α induces G2-arrest of cells after gamma irradiation.

体外研究

体内研究

30% Propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)

激酶实验

细胞实验

10 μM

动物实验

2.2 mg/kg 腹腔注射

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）

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。

参考文献

[1] Komarov PG, et al. Science, 1999, 285(5434), 1733-1737.
[2] Culmsee, C., et al., 2001. A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid beta-peptide. Journal of neurochemistry. 77(1): 220-8.
[3] Lorenzo, Elisa., et al., 2002. Doxorubicin induces apoptosis and CD95 gene expression in human primary endothelial cells through a p53-dependent mechanism. The Journal of biological chemistry. 277(13): 10883-92.
[4] Hoagland, Martin S., et al., 2005. The p53 inhibitor pifithrin-alpha is a potent agonist of the aryl hydrocarbon receptor. The Journal of pharmacology and experimental therapeutics. 314(2): 603-10.
[5] Sohn, D., et al., 2009. Pifithrin-alpha protects against DNA damage-induced apoptosis downstream of mitochondria independent of p53. Cell death and differentiation. 16(6): 869-78.

体内溶解度

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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