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生物活性
Go 6983 is a potent PKC inhibitor and has a different mechanism with the reported PKC inhibitor Ro-317549. When tested with MCF-7 and T47D cells, Go 6983 showed reversible effect on the down-regulation of PKCαand PKCδ induced by PKC activator PDBu, while decreased the expression of PKCη which up-regulated by PDBu. Further, Go 6983 treatment inhibited the MCF-7 cell survival by inhibiting the expression of PKCη. In ARCcPE cells, PMA treatment promoted the EMT process by up-regulating the expression of PKCs(PKCα, PKCβand PKCγ) which could be significantly inhibited by Go6983 treatment through inhibiting PKCs expression at the dose of 200 nM and completely inhibited at the dose of 1000 nM.
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体外研究
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体内研究
30% PEG400+0.5% Tween80+5% Propylene glycol
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激酶实验
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细胞实验
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动物实验
22 μg/mouse i.v.
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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] Gschwendt M, et al. FEBS Lett, 1996, 392(2), 77-80.
[2] Stempka, L., et al. 1997. J. Biol. Chem. 272: 6805-6811.
[3] Wang, D., et al. 1998. J. Biol. Chem. 273: 33027-33034.
分子式
C26H26N4O3 |
分子量
442.51 |
CAS号
133053-19-7 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
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DMSO
>50 mg/mL |
Water
<1 mg/mL |
Ethanol
<1 mg/mL |
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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