ChemicalBook > CAS DataBase List > GNE-493
GNE-493
GNE-493
- CAS No.1033735-94-2
- Chemical Name:GNE-493
- CBNumber:CB22621137
- Molecular Formula:C17H20N6O2S
- Formula Weight:372.44
- MOL File:1033735-94-2.mol
GNE-493 Property
- 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
- FDA UNII 0L843LS9YK
- Symbol(GHS)
- Signal word
- Hazard statements
- Precautionary statements
GNE-493 Chemical Properties,Usage,Production
- 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-493 Preparation Products And Raw materials
Raw materials
Preparation Products
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1033735-94-2, GNE-493Related Search:
- API
- 药靶配体
- 化工
- 细胞生物学试剂
- 抑制剂
- 化合物GNE-493,10 MM DMSO 溶液
- 2-(2-(2-氨基嘧啶-5-基)-4-吗啉噻吩[3,2-D]嘧啶-6-基)丙-2-醇
- 化合物GNE-493
- 双重泛PI3K/MTOR抑制剂(GNE-493)
- 2-(2-氨基-5-嘧啶基)-ALPHA,ALPHA-二甲基-4-(4-吗啉基)噻吩并[3,2-D]嘧啶-6-甲醇
- 1033735-94-2
- GNE-493, 10 mM in DMSO
- GNE493,Mammalian target of Rapamycin,PI3K,Inhibitor,inhibit,GNE-493,Phosphoinositide 3-kinase,mTOR,GNE 493
- Thieno[3,2-d]pyrimidine-6-methanol, 2-(2-amino-5-pyrimidinyl)-α,α-dimethyl-4-(4-morpholinyl)-
- 2-[2-(2-aminopyrimidin-5-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]propan-2-ol
- GNE 493;GNE493
- CS-1783
- 2-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[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-Amino-5-pyrimidinyl)-alpha,alpha-dimethyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidine-6-methanol
- GNE-493