WAY-600

WAY-600 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with IC50 of 9 nM for recombinant mTOR enzyme. It blocks mTOR complex 1/2 (mTORC1/2) assembly and activation.

• in vitro

  WAY-600 decreased 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 . Meanwhile, BrdU incorporation in HepG2 cells is also inhibited with WAY-600 treatment. It 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).

• 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, the in vivo anti-cancer activity by WAY-600 is further potentiated with the co-administration of MEK-162 (2.5 mg/kg, po daily).

• target

  mTOR 9 nM (IC 50 )

  mTORC1 < /span>

  mTORC2

  PI3K alpha 1.96 μM (IC 50 )

  PI3K gamma 8.45 μM (IC 50 )

WAY-600 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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