GNE-493
GNE-493 Basic information
- Product Name:
- GNE-493
- Synonyms:
-
- GNE-493
- 2-(2-Amino-5-pyrimidinyl)-alpha,alpha-dimethyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidine-6-methanol
- CS-1783
- GNE 493;GNE493
- 2-[2-(2-aminopyrimidin-5-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]propan-2-ol
- 2-(2-Amino-5-pyrimidinyl)-alpha,alpha-dimethyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidine-6-methanol GNE-493
- 2-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)propan-2-ol
- Thieno[3,2-d]pyrimidine-6-methanol, 2-(2-amino-5-pyrimidinyl)-α,α-dimethyl-4-(4-morpholinyl)-
- CAS:
- 1033735-94-2
- MF:
- C17H20N6O2S
- MW:
- 372.44
- Product Categories:
-
- API
- Mol File:
- 1033735-94-2.mol
GNE-493 Chemical Properties
- Density
- 1.408±0.06 g/cm3(Predicted)
- storage temp.
- Desiccate at -20°C
- solubility
- DMF:20.0(Max Conc. mg/mL);53.7(Max Conc. mM)
DMF:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.34(Max Conc. mM)
DMSO:45.0(Max Conc. mg/mL);120.82(Max Conc. mM)
Ethanol:1.1(Max Conc. mg/mL);2.95(Max Conc. mM) - pka
- 13.17±0.29(Predicted)
- form
- Powder
- color
- Off-white to gray
GNE-493 Usage And Synthesis
Uses
GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
in vivo
To confirm and compare in vivo efficacy, GNE-493 is examined in the human MCF7.1 breast cancer xenograft model that harbors a PI3Kα activating mutation. Mice bearing xenografts are dosed orally once daily with 10 mg/kg of GNE-493 for 21 continuous days. Similar to observations made in the PC3 prostate cancer xenograft model, 10 mg/kg of GNE-493 results in 73% tumor growth inhibition at day 21 when compared to vehicle control animals. When achieving comparable levels of drug exposure, GNE-493 shows a similar suppression of the PI3K pathway and consequently, a similar efficacy profile against MCF7.1 breast tumors[1].
IC 50
PI3Kα: 3.4 nM (IC50); PI3Kβ: 12 nM (IC50); PI3Kδ: 16 nM (IC50); PI3Kγ: 16 nM (IC50); mTOR: 30 nM (IC50)
References
[1] Sutherlin DP, 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. DOI:10.1021/jm901284w
GNE-493Supplier
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- sales@boylechem.com
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- 13817811078
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- 021-58950125
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- +86-021-50720296
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- +1 (866) 930-6790
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