PI-103 |
| カタログ番号GC11165 |
PI-103 は、p110α、p110β、p110δ、p110γ、mTORC1、および mTORC2 に対して 8 nM、88 nM、48 nM、150 nM、20 nM、および 83 nM の IC50 を持つ強力な PI3K および mTOR 阻害剤です。 PI-103 は、2 nM の IC50 で DNA-PK も阻害します。 PI-103 はオートファジーを誘導します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 371935-74-9
Sample solution is provided at 25 µL, 10mM.
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PI-103 is a potent and selective inhibitor of class I PI3K, mTOR and DNA-PK with IC50 values of 2, 3, 3, 15, 30 and 23 nM for p110α, p110β, p110δ, p110γ, mTOR and DNA-PK, respectively [1].
PI-103 showed potent antiproliferation activities in various cancer cell lines such as prostate, ovary and glioblastoma. It exerted GI50 values of 0.14, 0.06, 0.13, 0.10, 0.12 and 0.08 μM in U87MG, IGROV-1, DETROIT-562, PC3, SKOV-3 and HUVEC cells, respectively. In U87MG cells, 2 hour-treatment of PI-103 caused inhibition effects on various phosphorylated protein biomarkers of PI3K pathway with IC50 values of 15, 36, 111, 106 and 105 nM for p-AKTSer473, p-AKTThr308, p-GSK3βSer9, p-p70S6KThr421/Ser424 and p-S6RPSer235/Ser236, respectively [1].
References:
[1] Raynaud F I, Eccles S A, Patel S, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Molecular cancer therapeutics, 2009, 8(7): 1725-1738.
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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