| Identification | Back Directory | [Name]
GNE-490 | [CAS]
1033739-92-2 | [Synonyms]
GNE-490
CS-2657
GNE490;GNE 490
Thieno[3,2-d]pyrimidine-6-methanol, 2-(2-amino-4-methyl-5-pyrimidinyl)-α,α-dimethyl-4-(4-morpholinyl)-
2-(2-Amino-4-methyl-5-pyrimidinyl)-alpha,alpha-dimethyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidine-6-methanol | [Molecular Formula]
C18H22N6O2S | [MDL Number]
MFCD18251527 | [MOL File]
1033739-92-2.mol | [Molecular Weight]
386.47 |
| Hazard Information | Back Directory | [Description]
GNE-490 is a highly selective pan-PI3K inhibitor, demonstrating selectivity over mTOR. | [Uses]
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]. | [IC 50]
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. DOI:10.1021/jm901284w |
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| Company Name: |
Lynnchem
|
| Telephone: |
86-(0)29-85992781 17792393971 |
| Website: |
http://www.lynnchem.com/ |
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