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生物活性
PP2 is a potent Src family inhibitor that plays an important role in the cancer and is regarded as a promising target for treatment. When tested with human glioma cell line U251 spheroids in 3-D model, PP2 inhibited the cell invasion in a dose-dependent manner (2.5 μM, 10μM). And treated monolayer U251 cells with PP2 (10μM) decreased cell proliferation rate by inhibiting Src. In human T cells, PP2 showed inhibition on anti-CD3-induced tyrosine phosphorylation by inhibiting Lck and Fyn that involved in the early T cell signal transduction.
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体外研究
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体内研究
1% DMSO+30% polyethylene glycol+1% Tween 80
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激酶实验
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细胞实验
~100 μM
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动物实验
5 mg/kg/day 腹腔注射
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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] Hanke JH, et al. J Biol Chem, 1996, 271(2), 695-701.
[2] Salazar, E.P., et al. 1999. J. Biol. Chem. 274: 28371-28378.
[3] Bain, J., et al. 2003. Biochem. J. 371: 199-204.
[4] Bain, J., et al. 2003. Biochem. J. 371: 199-204.
[5] Liu, X., et al. 2010. FEBS Lett. 584: 3185-3192.
分子式
C15H16ClN5 |
分子量
301.77 |
CAS号
172889-27-9 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
|
DMSO
20 mg/mL |
Water
<1 mg/mL |
Ethanol
10 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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