GNE-293

Names

[ Name ]:
GNE-293

[Synonym ]:
9H-Purine, 9-methyl-2-[2-(1-methylethyl)-1H-benzimidazol-1-yl]-6-(4-morpholinyl)-8-[[1-(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)-3-azetidinyl]oxy]-
8-{[1-(1,1-Dioxidotetrahydro-2H-thiopyran-4-yl)-3-azetidinyl]oxy}-2-(2-isopropyl-1H-benzimidazol-1-yl)-9-methyl-6-(4-morpholinyl)-9H-purine

Biological Activity

[Description]:

GNE-293 is a potent and selective PI3Kδ inhibitor with Ki of 0.47 nM, displays 256, 420, 219-fold selectivity over PI3Kα, PI3Kβ, PI3Kγ, respectively; exhibits excellent potency in human whole blood (HWB) assay (CD69 HWB IC50=4.38 nM); possesses favorable pharmacokinetic properties and orally bioavailable.

[References]

References 1. Safina BS, et al. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4953-9. View Related Products by Target PI3K

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
853.5±75.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₈H₃₆N₈O₄S

[ Molecular Weight ]:
580.702

[ Flash Point ]:
470.0±37.1 °C

[ Exact Mass ]:
580.257996

[ LogP ]:
1.20

[ Vapour Pressure ]:
0.0±3.2 mmHg at 25°C

[ Index of Refraction ]:
1.755

Related Compounds

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