A pan inhibitor of PI3Ks and an inhibitor of mTOR
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Bimiralisib

Item No. 23441

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)-2-pyridinamine
CAS Number
1225037-39-7
Synonyms
  • PI3K-IN-2
Molecular Formula
C17H20F3N7O2
Formula Weight
411.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 2 mg/ml
λmax
203, 233, 279 nm
SMILES
NC(N=C1)=CC(C(F)(F)F)=C1C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2
InChi Code
InChI=1S/C17H20F3N7O2/c18-17(19,20)12-9-13(21)22-10-11(12)14-23-15(26-1-5-28-6-2-26)25-16(24-14)27-3-7-29-8-4-27/h9-10H,1-8H2,(H2,21,22)
InChi Key
ADGGYDAFIHSYFI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Bimiralisib is a potent and orally bioavailable inhibitor of phosphatidylinositol 3-kinases (PI3Ks; IC50s = 33, 661, 708, and 451 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively) and the mammalian target of rapamycin (mTOR; IC50 = 89 nM).1 It is selective for these kinases over a panel of cell surface and nuclear receptors, membrane channels, transporters, kinases, proteases, and phosphodiesterases at a concentration of 10 μM. Bimiralisib has anticancer activity with an average GI50 value of 0.7 μM across the National Cancer Institute (NCI) 60 human cancer cell line panel. In vivo, bimiralisib (5-15 mg/kg) reduces tumor growth in a dose-dependent manner in a PC3 prostate cancer mouse xenograft model. Formulations containing bimiralisib are under clinical investigation for the treatment of relapsed and refractory lymphoma and advanced solid tumors.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Beaufils, F., Cmiljanovic, N., Cmiljanovic, V., 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. 60(17), 7524-7538 (2017).