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GNE-490

Product Specifications

UNSPSC Description

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].

Target Antigen

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 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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, protect from light)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-10812/GNE-490-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-10812/GNE-490-SDS-MedChemExpress.pdf

Clinical Information

No Development Reported

CAS Number

1033739-92-2

Available Sizes

Curated Selection

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