PQR530

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].

Product Specifications

CAS Number

[1927857-61-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

MTOR; PI3K

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PQR-530.html

Purity

99.85

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

FC(C1=CC(N)=NC=C1C2=NC(N3CCOCC3)=NC(N4[C@H](COCC4)C)=N2)F

Molecular Formula

C18H23F2N7O2

Molecular Weight

407.42

Precautions

H302, H315, H319, H335

References & Citations

[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) :6241-6261.