"目錄號: HY-15272
WAY-600是有效，ATP競爭型遮婶，選擇性的mTOR抑制劑蹋艺，抑制重組mTOR酶的IC50值為9 nM。
相關(guān)產(chǎn)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
