PI3Kα-IN-29

PI3Kα-IN-29 is a potent, orally active and selective PI3Kα with an IC50 of 2.5 nM. PI3Kα-IN-29 exhibits >400-fold selectivity over PI3Kβ/δ/γ/mTOR. PI3Kα-IN-29 selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses PI3K/AKT/mTOR signaling, induces G1 arrest, and inhibits migration. PI3Kα-IN-29 inhibits tumor growth in a T47 mouse model. PI3Kα-IN-29 can be used for the research of breast cancer[1].

Product Specifications

UNSPSC

12352005

Target

Akt; Cadherin; CDK; mTOR; PI3K

Related Pathways

Cell Cycle/DNA Damage; Cytoskeleton; PI3K/Akt/mTOR

Field of Research

Cancer

Smiles

C[C@H](OC1=CC=C2C3=NC(C4=CC5=C(C=C4)OC(N)=N5)=CN3COC2=C1)C(N)=O

Molecular Formula

C20H17N5O4

Molecular Weight

391.38

References & Citations

[1]Hou Y, et al. Structure-Guided Design of a Highly Selective PI3Kα Inhibitor Overcoming Metabolic Dysregulation with Potent Anti-breast Cancer Efficacy. J Med Chem. 2025;68 (22) :24404-24423.