PI3Kα-IN-22

PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3KαH1047R, with an IC50 of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice[1].

Product Specifications

CAS Number

[2925030-26-6]

UNSPSC

12352005

Target

PI3K

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pi3kα-in-22.html

Solubility

10 mM in DMSO

Smiles

CC(C=C([C@H](NC1=CC=CC=C1C(O)=O)C)C2=NC(N3CCC(F)(F)CC3)=C4C#N)=CN2C4=O

Molecular Formula

C24H23F2N5O3

Molecular Weight

467.47

References & Citations

[1]Ketcham JM, et al. Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein. J Med Chem. 2024 Mar 28;67 (6) :4936-4949.