Bimiralisib

• Description :

  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 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

• CAS Number :

  [1225037-39-7]