生物活性

PD98059 treatment resulted in distinct changes in cell morphology and density compared to control cells treated with DMSO. PD98059 inhibited proliferation or induced cell death in human leukemic U937 cells. Additionally, PD98059 dose-dependently inhibited the ERK1/2 phosphorylation as well as down-regulated cyclin E/Cdk2 and cyclin D1/Cdk4 levels, resulting in G1 phase arrest and apoptosis induction in U937 cells.

体外研究

体内研究

30% PEG400+0.5% Tween80+5% Propylene glycol

激酶实验

细胞实验

~100 μM

动物实验

10 mg/kg 静脉注射

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] Dudley DT, et al. Proc Natl Acad Sci U S A, 1995, 92(17), 7686-7689.
[2] Pang, L., et al., 1995. Inhibition of MAP kinase kinase blocks the differentiation of PC-12 cells induced by nerve growth factor. The Journal of biological chemistry. 270(23): 13585-8.
[3] Badache, A., et al., 2001. Interleukin 6 inhibits proliferation and, in cooperation with an epidermal growth factor receptor autocrine loop, increases migration of T47D breast cancer cells. Cancer research. 61(1): 383-91.
[4] Kang, Keon Wook., et al., 2003. Activation of CCAAT/enhancer-binding protein beta by 2'-amino-3'-methoxyflavone (PD98059) leads to the induction of glutathione S-transferase A2. Carcinogenesis. 24(3): 475-82.
[5] Kim, Sang K., et al., 2006. The mitogen-activated protein kinase kinase (mek) inhibitor PD98059 elevates primary cultured rat hepatocyte glutathione levels independent of inhibiting mek. Drug metabolism and disposition: the biological fate of chemicals. 34(4): 683-9.
[6] Kojima, Kensuke., et al., 2007. Mitogen-activated protein kinase kinase inhibition enhances nuclear proapoptotic function of p53 in acute myelogenous leukemia cells. Cancer research. 67(7): 3210-9.

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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