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GNE-493 is potent, selective, and orally available PI3K and mTOR inhibitor with potential anticancer activity.IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR,respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $41 | In Stock | |
5 mg | $106 | In Stock | |
10 mg | $172 | In Stock | |
25 mg | $363 | In Stock | |
50 mg | $579 | In Stock | |
100 mg | $892 | In Stock | |
1 mL x 10 mM (in DMSO) | $117 | In Stock |
Description | GNE-493 is potent, selective, and orally available PI3K and mTOR inhibitor with potential anticancer activity.IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR,respectively. |
Targets&IC50 | PI3Kγ:16 nM , mTOR:32 nM, PI3Kα:3.4 nM , PI3Kδ:16 nM , PI3Kβ:12 nM |
In vivo | GNE-493 was tested in a human MCF7.1 breast cancer xenograft model with a PI3Kα activating mutation. Mice with xenografts received a daily oral dose of 10 mg/kg of GNE-493 for 21 continuous days. Comparable to results in the PC3 prostate cancer model, this treatment led to a 73% inhibition of tumor growth by day 21 compared to control. With similar drug exposure levels, GNE-493 demonstrated equivalent suppression of the PI3K pathway and, thus, comparable efficacy against MCF7.1 breast tumors. |
Molecular Weight | 372.44 |
Formula | C17H20N6O2S |
Cas No. | 1033735-94-2 |
Smiles | CC(C)(O)c1cc2nc(nc(N3CCOCC3)c2s1)-c1cnc(N)nc1 |
Relative Density. | 1.408 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (120.82 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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