Bimiralisib

Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.

Product Specifications

CAS Number

[1225037-39-7]

Product Name Alternative

PQR309

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/PQR309.html

Purity

98.62

Solubility

DMSO : ≥ 50 mg/mL

Smiles

NC1=NC=C(C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)C(C(F)(F)F)=C1

Molecular Formula

C17H20F3N7O2

Molecular Weight

411.38

Precautions

H302, H315, H319, H335

References & Citations

[1]Beaufils F, et al. 5- (4,6-Dimorpholino-1,3,5-triazin-2-yl) -4- (trifluoromethyl) pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. J Med Chem. 2017 Sep 14;60 (17) :7524-7538.|[2]Wicki A, et al. First-in human, phase 1, dose-escalation pharmacokinetic and pharmacodynamic study of the oral dual PI3K and mTORC1/2 inhibitor PQR309 in patients with advanced solid tumors (SAKK 67/13) . Eur J Cancer. 2018 Jun;96:6-16.