生物活性

LY294002 is a potent inhibitor of PI 3-kinase, a protein in the phosphoinositide 3-kinase family of intercellular signal regulating enzymes. Reports indicate that LY294002 encourages apoptosis in such cells by blocking the PI 3-kinase/Akt signaling pathway which has been strongly related to cancer survival and proliferation. This compound is selective for PI 3-kinase p110 β (PI 3-Kβ) and PI 3-kinase p110 α (PI 3-Kα), although it will inhibit other PI 3 kinases at higher concentrations (IC50 = 310 nM and 730 nM for PI 3-Kβ and PI 3-Kα, respectively). The pathway associated with these receptors is implicated in cancer and diabetes, and LY294002 is an important tool for studying this relationship.

体外研究

体内研究

2% DMSO+30% polyethylene glycol+1% Tween 80

激酶实验

细胞实验

0–50 μM

动物实验

0–100 mg/kg Administered via i.p.

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] Chaussade C, et al. Biochem J, 2007, 404(3), 449-58.
[2] Gagnon, A., et al. 2001. Endocrinology. 142: 205-212.
[3] Semba, S. et al. 2002. Clin. Cancer Res. 8(6): 1957-1963.
[4] Cantley, L.C., 2002. Science. 296: 1655-1657.
[5] Chaussade, C. et al. 2007. Biochem. J. 404(3): 449-458.
[6] Sapey, E. et al. 2014. Blood. 123(2): 239-248.
[7] Gardner, E.E. et al. 2014. Cancer Res. 74(10): 2846-2856.
[8] Bolen, C.R. et al. 2014. Hepatology. 59(4): 1262-1272.
[9] Mbengue, A. et al. 2015. Nature. 520(7549): 683-687.
[10] Malin, D. et al. 2015. Oncogene. 34(45): 5626-5634.

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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