产品描述:
PQR530 is a dual inhibitor of PI3Kα and mammalian target of rapamycin (mTOR; IC50s = 11.1 and 7.4 nM, respectively).{50007} It inhibits phosphorylation of Akt and ribosomal S6 kinase in A2058 melanoma cells (IC50s = 62.2 and 61.1 nM, respectively). PQR530 inhibits cell growth in a panel of 66 cancer cell lines (mean GI50 = 0.43 µM). In vivo, PQR530 (25 mg/kg) reduces tumor growth in an OVCAR-3 ovarian cancer mouse xenograft model. It decreases the number of seizures per week in a Tsc1GFAP conditional knockout mouse model of epilepsy.{58361}