PQR530 Chemical Properties

Boiling point:

660.7±65.0 °C(Predicted)

Density 

1.338±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:3): 0.33 mg/ml; DMSO: 10 mg/ml

form 

A crystalline solid

pka

5.05±0.10(Predicted)

color 

Light yellow to yellow

PQR530 Usage And Synthesis

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

PQR530(1927857-61-1)Related Product Information

• PPQ-102
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• 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine