WAY-600

"目录号: HY-15272

PI3K/Akt/mTOR-

WAY-600是有效，ATP竞争型，选择性的mTOR抑制剂，抑制重组mTOR酶的IC50值为9 nM。

mTOR

相关产品

Rapamycin-Everolimus-AP1903-INK-128-BEZ235-Torin 1-AP20187-AZD-8055-MHY1485-PP 242-LY3023414-AZD2014-PF-04691502-Temsirolimus-Torin 2-

生物活性

Description

WAY-600 is a potent, ATP-competitive, and selectivemTORinhibitor with anIC50of 9 nM for recombinant mTOR enzyme.

IC50& Target

IC50: 9 nM (mTOR)[1]

In Vitro

WAY-600 exhibits a concentration-dependent and time-dependent inhibition of f HepG2 and Huh-7 cells viability. Following WAY-600 (1-1000 nM) treatment, the number of HepG2 cell colonies is dramatically decreased. Meanwhile, BrdU incorporation in HepG2 cells is also inhibited with WAY-600 treatment. WAY-600 dose-dependently increases the activity of caspase-3 and caspase-9 in HepG2 cells. WAY-600 disrupts assemble of mTORC1 (mTOR-Raptor association) and mTORC2 (mTOR-Rictor association). Activation of mTORC1 (indicated by p-S6K1 and p-4E-BP1) and mTORC2 is almost blocked by WAY-600 (100 nM)[2].

In Vivo

Administration of WAY-600 (10 mg/kg, daily) inhibits HepG2 tumor growth in nude mice. Daily HepG2 tumor growth of WAY-600-administrated mice is significantly lower than that of vehicle control mice. Importantly, thein vivoanti-cancer activity by WAY-600 is further potentiated with the co-administration of MEK-162 (2.5 mg/kg, p.o. daily)[2].

References

[1].Yu K, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 2009 Aug 1;69(15):6232-40.

[2].Wang K, et al. MEK-ERK inhibition potentiates WAY-600-induced anti-cancer efficiency in preclinical hepatocellular carcinoma (HCC) models. Biochem Biophys Res Commun. 2016 May 27;474(2):330-7.