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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
MTOR; mTORC1; mTORC2; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ; Vps34
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