GNE-493


CAS No. : 1033735-94-2

GNE-493,1033735-94-2
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000200
Synonyms:2-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)propan-2-ol
Molecular Formula:C17H20N6O2S
Molecular Weight:372.44
Target:mTOR
IC50:3.4/12/16/16/32 nM(PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR) [1]
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Appearance:Solid powder
Purity: > 98%
Cat No:I000200
Cas No:1033735-94-2
Product-Name:GNE-493

GNE-493 is a potent, selective, and orally available dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/12/16/16/32 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR respectively.
IC50 value: 3.4/12/16/16/32 nM(PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR) [1]
Target: pan-PI3K/mTOR inhibitor
GNE-493 has good pharmacokinetic (PK) parameters, GNE-493 is highly selective, demonstrate knock down of pathway markers in vivo, and are efficacious in xenograft models where the PI3K pathway is deregulated. GNE-493 was compared in a PI3KR mutated MCF7.1 xenograft model and were found to have equivalent efficacy when normalized for exposure.


[1]. Sutherlin DP, 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.

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