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GNE-317

Chemical Structure : GNE-317

CAS No.: 1394076-92-6

GNE-317 (GNE317)

Catalog No.: PC-43188Not For Human Use, Lab Use Only.

GNE-317 (GNE317) is a potent, brain penepenetrant, dual PI3K/mTOR inhibitor having physicochemical properties predictive of low efflux by P-gp and BCRP.

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Biological Activity

GNE-317 (GNE317) is a potent, brain penepenetrant, dual PI3K/mTOR inhibitor having physicochemical properties predictive of low efflux by P-gp and BCRP.
GNE-317 inhibits the cell proliferation of GBM6, 10, 22, and 84 with IC50 of 0.59, 0.72, 0.26, and 3.49 uM, respectively.
GNE-317 markedly inhibits the PI3K pathway in mouse brain, causing 40% to 90% suppression of the pAkt and pS6 signals.
GNE-317 significantly inhibits tumor growth in orthotopic models of glioblastoma multiforme (GBM).

Physicochemical Properties

M.Wt 414.4814
Formula C19H22N6O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 20 mg/mL

Chemical Name/SMILES

2-Pyrimidinamine, 5-[6-(3-methoxy-3-oxetanyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-

References

1. Salphati L, et al. Clin Cancer Res. 2012 Nov 15;18(22):6239-48.

2. Lewis Phillips GD, et al. Breast Cancer Res Treat. 2017 Aug;164(3):581-591.

3. Becker CM, et al. Neuro Oncol. 2015 Sep;17(9):1210-9.

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