GNE-490

GNE-490, a (thienopyrimidin-2-yl) aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM) . GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model[1].

Product Specifications

CAS Number

[1033739-92-2]

UNSPSC

12352005

Target

MTOR; PI3K

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gne-490.html

Purity

96.29

Solubility

DMSO : ≥ 100 mg/mL

Smiles

OC(C)(C)C1=CC(N=C(C2=CN=C(N)N=C2C)N=C3N4CCOCC4)=C3S1

Molecular Formula

C18H22N6O2S

Molecular Weight

386.47

References & Citations

[1]Daniel P Sutherlin, et al. Discovery of (thienopyrimidin-2-yl) aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. J Med Chem. 2010 Feb 11;53 (3) :1086-97.