PQR620

PQR620 is an inhibitor of mTOR (K_i = 10.8 nM).¹ It is selective for mTOR over PI3K p110α (K_i = 4.2 µM) and a panel of 456 other kinases at 10 µM. PQR620 has antiproliferative activity against a panel of 66 cancer cell lines (mean IC₅₀ = 919 nM). It induces cell cycle arrest at the G₁ phase in A2058 melanoma and SKOV3 ovarian cancer cells when used at a concentration of 5 µM. In vivo, PQR620 (100 mg/kg per day) decreases the number of seizures per week in a Tsc1^GFAP conditional knockout mouse model of epilepsy to a similar extent as PQR530 (Item No. 28563).²

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1. Rageot, D., Bohnacker, T., Melone, A., et al. Discovery and preclinical characterization of 5-[4,6-bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a highly potent and selective mTORC1/2 inhibitor for cancer and neurological disorders. J. Med. Chem. 61(22), 10084-10105 (2018).

2. Theilmann, W., Gericke, B., Schidlitzki, A., et al. Novel brain permeant mTORC1/2 inhibitors are as efficacious as rapamycin or everolimus in mouse models of acquired partial epilepsy and tuberous sclerosis complex. Neuropharmacology 180, 108297 (2020).