PI3Kα/mTOR-IN-1 |
| Katalog-Nr.GC36909 |
PI3Kα/mTOR-IN-1 ist ein potenter PI3Kα/mTOR dualer Inhibitor mit einem IC50 von 7 nM fÜr PI3Kα in einem Zellassay und Kis von 10,6 nM und 12,5 nM fÜr mTOR und PI3Kα in einem zellfreien Assay.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1013098-90-2
Sample solution is provided at 25 µL, 10mM.
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PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively. PI3Kα|7 nM (IC50, Cell Assay)|PI3Kα|12.5 nM (Ki)|mTOR|10.6 nM (Ki)
PI3Kα/mTOR-IN-1 exhibits potent activity against PI3Kα and mTOR, high LipE, good kinase selectivity and robust ADMET properties[1].
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 Vdss, T1/2 of 0.9 h, and good oral bioavailability[1].
[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.
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