GNE-317 GNE-317 is a potent, brain-penetrant PI3K inhibitor.
Targets
PI3K
In vitro
GNE-317 is not a substrate of P-gp or BCRP transporter in transfected Madin-Darby canine kidney (MDCK) cells. Binding of GNE-317 to plasma proteins exhibits a free fraction of 14.9 % in mouse plasma, and binding to brain tissues is higher, with a free fraction of 5.4%. GNE-317 shows cytostasis but no cell death to U87 cells.
In vivo
GNE-317 (40 mg/kg, p.o.) markedly inhibits the PI3K pathway in mouse brain, causing 40% to 90% suppression of the pAkt and pS6 signals up to 6-hour postdose. GNE-317 (40 mg/kg, p.o.) is efficacious in the U87 and GS2 orthotopic models, achieving tumor growth inhibition of 90% and 50%, respectively. In the GBM10 tumor model, GNE-317 (30 mg/kg, p.o.; 40 mg/kg the first 2 weeks) extends the survival of mice from a median of 55.5 to 75 days.
GNE-317 is an orally active potent inhibitor against phosphoinositide 3-kinase (PI3K Ki = 2/α, 27/β, 7/δ, 7/γ) and mTOR (Ki = 9 nM). GNE-317 exhibits antiproliferation potency in glioblastoma cancer cultures (EC50 from 140 to 570 nM in seven cultures) and
Storage
Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
This compound belongs to the class of organic compounds known as bipyrimidines and oligopyrimidines. These are organic compounds containing two or more pyrimidine rings directly linked to each other. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
Solubility (25°C) In vitro DMSO: 47 mg/mL warmed with 50ºC Water: bath (113.39 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility
47
DMSO(mM) Max Solubility
113.3950975
Water(mg / mL) Max Solubility
＜1
Molecular Weight
414.500 g/mol
XLogP3
0.500
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
10
Rotatable Bond Count
4
Exact Mass
414.147 Da
Monoisotopic Mass
414.147 Da
Topological Polar Surface Area
137.000 Ų
Heavy Atom Count
29
Formal Charge
0
Complexity
570.000
Isotope Atom Count
0
Defined Atom Stereocenter Count
0
Undefined Atom Stereocenter Count
0
Defined Bond Stereocenter Count
0
Undefined Bond Stereocenter Count
0
The total count of all stereochemical bonds
0
Covalently-Bonded Unit Count
1
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