NV-128 (LY-303511) is a novel isoflavone derivative that inhibits mTOR and promotes caspase-independent cell death; induce significant cell death in both paclitaxel-resistant and carboplatin-resistant EOC cells with GI50 of 1-5 ug/mL; significantly depresses mitochondrial function by decrease in ATP, Cox-I, and Cox-IV levels, and by increase in mitochondrial superoxide and hydrogen peroxide.
RapaLink-1 is a third-generation mTOR inhibitor that overcomes resistance to existing first- and second-generation inhibitors; blocks mTOR signaling of the F2108L mTOR and M2327I mTOR drug resistant mutants; RapaLink-1 is more potent mTOR inhibitor than rapamycin.
Seco Rapamycin sodium salt
Seco-rapamycin is the first in vivo open-ring metabolite of rapamycin that does not affect mTOR.
PQR-620 (PQR620) is a novel potent and selective, brain penetrant inhibitor of mTORC1/2; displays >1000-fold selectivity towards mTOR over PI3Kα in enzymatic binding assays; demonstrates inhibition of protein kinase B (pSer473) and ribosomal protein S6 (pSer235/236) phosphorylation with IC50 of 0.2 uM and 0.1 uM, respectively; shows anti-tumor effects in vitro and in vivo.
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