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| | GNE 477 Basic information |
| Product Name: | GNE 477 | | Synonyms: | GNE 477;5-[7-Methyl-4-(Morpholin-4-yl)-6-[(4-Methylsulfonylpiperazin-1-yl)Methyl]thieno[3,2-d]pyriMidin-2-yl]pyriMidin-2-aMine;5-[7-Methyl-4-(morpholin-4-yl)-6-[(4-methylsulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-2-yl]pyrimidin-2-amine GNE 477;5-(7-Methyl-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-;CS-1884;2-Pyrimidinamine, 5-[7-methyl-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-;5-(7-Methyl-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine;mTOR,Phosphoinositide 3-kinase,GNE-477,Inhibitor,Mammalian target of Rapamycin,GNE477,inhibit,PI3K | | CAS: | 1032754-81-6 | | MF: | C21H28N8O3S2 | | MW: | 504.63 | | EINECS: | | | Product Categories: | | | Mol File: | 1032754-81-6.mol |  |
| | GNE 477 Chemical Properties |
| density | 1.51±0.1 g/cm3(Predicted) | | storage temp. | Desiccate at -20°C | | solubility | insoluble in H2O; insoluble in EtOH; ≥16.69 mg/mL in DMSO with gentle warming | | form | Powder | | pka | 4.22±0.10(Predicted) |
| | GNE 477 Usage And Synthesis |
| Biological Activity | gne-477 is a potent dual pi3k/mtor inhibitor. owing to the common association with oncogenic malignancies, the pi3k/akt/mtor signaling pathway is regarded as an attractive area of research for the identification of oral small molecule inhibitors. | | in vitro | gne-477 was found to inhibit pi3k-α, β, δ, and γ with ic50s of 4, 86, 6, and 15 nm, respectively. [1]. | | in vivo | a direct comparison of gne-477 with its des-methyl analog revealed that the trend of reduced in vivo clearance in rats is also observed in dogs and mice. the clearance improvement was significant in dogs where the des-methyl analog was cleared at two-thirds the rate of hepatic blood flow while gne-477 had low clearance. in an study evaluating the tumor growth inhibition of a pc3 tumor xenograft10 over 14 days, stasis was achieved at a 20 mg/kg qd dose of gne-477 and significant inhibition was found with doses as low as 1 mg/kg qd. gne-477 was generally well tolerated during this study as shown by acceptable levels of weight loss comparable to that in the vehicle cohort [1]. | | IC 50 | 4 and 21 nmol/l for pi3k and mtor, respectively | | references | [1] heffron tp,berry m,castanedo g,chang c,chuckowree i,dotson j,folkes a,gunzner j,lesnick jd,lewis c,mathieu s,nonomiya j,olivero a,pang j,peterson d,salphati l,sampath d,sideris s,sutherlin dp,tsui v,wan nc,wang s,wong s,zhu by. identification of gne-477, a potent and efficacious dual pi3k/mtor inhibitor. bioorg med chem lett.2010 apr 15;20(8):2408-11. |
| | GNE 477 Preparation Products And Raw materials |
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