GNE-490

Names

[ Name ]:
GNE-490

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
595.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₈H₂₂N₆O₂S

[ Molecular Weight ]:
386.47

[ Flash Point ]:
313.9±32.9 °C

[ Exact Mass ]:
386.152496

[ PSA ]:
139.25000

[ LogP ]:
1.48

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.676

[ Storage condition ]:
2-8℃

Related Compounds

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