PQR530

Uses

PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity[1][2].

IC 50

mTOR: 0.33 nM (Kd); PI3Kα: 0.84 nM (Kd); PI3Kβ: 6.1 nM (Kd); PI3Kγ: 10 nM (Kd); PI3Kδ: 11 nM (Kd); PI3KC2β: 100 nM (Kd)

References

[1] Denise Rageot, et al. Abstract 140: Discovery and biological evaluation of PQR530, a highly potent dual pan-PI3K/mTORC1/2 inhibitor. Cancer Res 2017;77(13 Suppl).
[2] Rageot D, et al. (S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase. J Med Chem. 2019;62(13):6241-62 DOI:10.1021/acs.jmedchem.9b00525