產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 25mg 100mg
CAS	371935-79-4
別名	PI 103 hydrochloride;PI103 hydrochloride
化學(xué)名	3-(4-morpholin-4-ylpyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenol;hydrochloride
分子式	C19H17ClN4O3
分子量	384.82
溶解度	≥ 19.25 mg/mL in DMSO
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

PI-103 is a dual inhibitor of PI3K/Akt and mTOR with IC50 value of 0.002 μM , 0.003μM, 0.003μM, 0.015μM, 0.030μM for P110α, P110β, P110γ, P110 and mTOR, respectively [1].

PI3K/AKT/mTOR pathway is an intracellular signaling pathway and plays an important role in regulating cell cycle. It has been shown that PI3K/AKT/MTOR pathway is directly related to cellular quiescence, proliferation, cancer, and longevity. And many studies have shown that activation of the PI3K/Akt signaling pathway is correlated with poor prognosis in a variety of cancers which demonstrated that inhibition of the pathway may be regarded as a promising therapy [2, 3].

PI-103 is a selective PI3K/Akt and mTORC1 inhibitor. When tested with leukemic cell lines (MOLM14, OCI-AML3 and MV4-11) with activation of PI3K/Akt, mTORC1 and ERK/MAPK signaling pathways, PI-103 blocked cells proliferation via inhibiting PI3K/Akt and mTORC1 activity in a concentration of 1μM [4]. In HCC cell line--Huh7 cells, treated PI-103 alone or combined with sorafenib inhibited cells proliferation in a dose-dependent manner through inhibition of PI3K/Akt and mTORC1 pathways [5]. When tested with U87MG glioblastoma cells, PI-103 treatment in 30 nM/L showed significant inhibition of PI3K/Akt and mTORC1 phosphorylation [1]. In neuroblastoma cell lines SK-N-BE (2), IMR-32 with amplified MYCN, PI-103 inhibited cell growth in a time- and concentration-dependent manner via inhibiting PI3K/Akt and mTORC1 activity [3].

In SK-N-BE (2) with MYCN-mutant xenografted nude mice model, treated PI-103 intraperitoneally (10 mg/kg) markedly reduced the tumor volume index and tumor weight via inhibiting PI3K/ mTOR pathways [1].

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1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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