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
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
PI3Kβ
Available Sizes
Frequently Asked Questions
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