PI3K/mTOR Inhibitor-9 

PI3K/mTOR Inhibitor-9 (Compound 1) is a potent mTOR and PI3K inhibitor with IC₅₀ values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM against mTOR (phospho-S6 cellular assay), PI3Kα, PI3Kγ and PI3Kδ, respectively^[1].

PI3K/mTOR Inhibitor-9 (Compound 1) shows good selectivity over the related kinases PI3Kα, β and γ, although with lower selectivity over PI3Kδ^[1].
PI3K/mTOR Inhibitor-9 inhibits CYP2D6 (IC₅₀ = 1.98 μM) and shows time-dependent inhibition (TDI) of CYP3A4 (rate of enzyme inhibition, k_obs = 0.080 /min)^[1].
PI3K/mTOR Inhibitor-9 shows good permeability with no sign of P-gp efflux (B-A/A-B: 0.95) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

433.51

C₂₃H₂₇N₇O₂

1392421-71-4

C[C@H]1N(CCOC1)C2=C3C(N=C(C4=C5C(NC=C5)=CC=C4)N3)=NC(N6[C@H](COCC6)C)=N2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Bonazzi S, et al. Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders. J Med Chem. 2020 Feb 13;63(3):1068-1083.  [Content Brief]