GNE-490

Modify Date: 2024-01-02 12:53:16

GNE-490 Structure
GNE-490 structure
Common Name GNE-490
CAS Number 1033739-92-2 Molecular Weight 386.47
Density 1.4±0.1 g/cm3 Boiling Point 595.3±60.0 °C at 760 mmHg
Molecular Formula C18H22N6O2S Melting Point N/A
MSDS N/A Flash Point 313.9±32.9 °C

 Use of GNE-490


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].

 Names

Name 2-[2-(2-Amino-4-methyl-5-pyrimidinyl)-4-(4-morpholinyl)thieno[3,2 -d]pyrimidin-6-yl]-2-propanol
Synonym More Synonyms

 GNE-490 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
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℃

 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
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