1033739-92-2

1033739-92-2 structure

Name: GNE-490
Chemical Name: 2-[2-(2-Amino-4-methyl-5-pyrimidinyl)-4-(4-morpholinyl)thieno[3,2 -d]pyrimidin-6-yl]-2-propanol
CAS Number: 1033739-92-2
Molecular Formula: C₁₈H₂₂N₆O₂S
Molecular Weight: 386.47
Catalog: Signaling Pathways PI3K/Akt/mTOR mTOR
Create Date: 2017-04-28 20:30:05
Modify Date: 2024-01-02 12:53:16
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].

Name	2-[2-(2-Amino-4-methyl-5-pyrimidinyl)-4-(4-morpholinyl)thieno[3,2 -d]pyrimidin-6-yl]-2-propanol
Synonyms	3,6,9,12,15,18-Hexaoxanonacosan-1-ol Thieno[3,2-d]pyrimidine-6-methanol, 2-(2-amino-4-methyl-5-pyrimidinyl)-α,α-dimethyl-4-(4-morpholinyl)- alcohol ethoxylate 2-[2-(2-Amino-4-methyl-5-pyrimidinyl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]-2-propanol

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].
Related Catalog	Signaling Pathways >> PI3K/Akt/mTOR >> mTOR Research Areas >> Cancer Signaling Pathways >> PI3K/Akt/mTOR >> PI3K
Target	PI3Kα:3.5 nM (IC50) PI3Kβ:25 nM (IC50) PI3Kδ:5.2 nM (IC50) PI3Kγ:15 nM (IC50) mTOR:750 nM (IC50)
References	[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.