GSK2636771

GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

Product Specifications

CAS Number

[1372540-25-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

PI3K

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GSK2636771.html

Purity

99.59

Solubility

DMSO : 16.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC1=NC2=C(C(O)=O)C=C(C=C2N1CC3=CC=CC(C(F)(F)F)=C3C)N4CCOCC4

Molecular Formula

C22H22F3N3O3

Molecular Weight

433.42

Precautions

H302, H315, H319, H335

References & Citations

[1]Weigelt B, et al. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res. 2013, 19 (13), 3533-3544.|[2]Hosford SR, et al. Combined inhibition of both p110α and p110β isoforms of phosphatidylinositol 3-kinase is required for sustained therapeutic effect in PTEN-deficient, ER+ breast cancer. Clin Cancer Res. 2016 Nov 30