PI3Kα/mTOR-IN-1 

PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC₅₀ of 7 nM for PI3Kα in a cell assay, and K_is of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.

PI3Kα/mTOR-IN-1 exhibits potent activity against PI3Kα and mTOR, high LipE, good kinase selectivity and robust ADMET properties^[1].

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

PI3Kα/mTOR-IN-1 exhibits low HLM ER, but it is highly cleared in rat liver microsome (RLM) with ER of 0.88. PI3Kα/mTOR-IN-1 exhibits moderate clearance, moderate V_dss, T_1/2 of 0.9 h, and good oral bioavailability^[1].

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

310.35

C₁₆H₁₈N₆O

1013098-90-2

Solid

Off-white to light yellow

O=C1C(C2=CNN=C2)=CC3=C(C)N=C(N)N=C3N1C4CCCC4

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Le PT, et al. Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR. Bioorg Med Chem Lett. 2012 Aug 1;22(15):5098-103.  [Content Brief]