PI3Kα/mTOR-IN-1

Modify Date: 2024-01-14 11:58:56

PI3Kα/mTOR-IN-1 Structure
PI3Kα/mTOR-IN-1 structure
Common Name PI3Kα/mTOR-IN-1
CAS Number 1013098-90-2 Molecular Weight 310.35
Density N/A Boiling Point N/A
Molecular Formula C16H18N6O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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 Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.

 Names

Name PI3Kα/mTOR-IN-1

 PI3Kα/mTOR-IN-1 Biological Activity

Description 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.
Related Catalog
Target

PI3Kα:7 nM (IC50, Cell Assay)

PI3Kα:12.5 nM (Ki)

mTOR:10.6 nM (Ki)

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

[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.

 Chemical & Physical Properties

Molecular Formula C16H18N6O
Molecular Weight 310.35