GNE 477
- Product Name
- GNE 477
- CAS No.
- 1032754-81-6
- Chemical Name
- GNE 477
- Synonyms
- GNE 477;CS-1884;5-(7-Methyl-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-;mTOR,Phosphoinositide 3-kinase,GNE-477,Inhibitor,Mammalian target of Rapamycin,GNE477,inhibit,PI3K;5-(7-Methyl-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[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;2-Pyrimidinamine, 5-[7-methyl-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-;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
- CBNumber
- CB62621135
- Molecular Formula
- C21H28N8O3S2
- Formula Weight
- 504.63
- MOL File
- 1032754-81-6.mol
GNE 477 Property
- 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)
- color
- Light yellow to yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H317May cause an allergic skin reaction
H319Causes serious eye irritation
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 27977
- Product name
- GNE-477
- Packaging
- 25mg
- Price
- $667
- Updated
- 2024/03/01
- Product number
- 27977
- Product name
- GNE-477
- Packaging
- 50mg
- Price
- $1018
- Updated
- 2024/03/01
- Product number
- 27977
- Product name
- GNE-477
- Packaging
- 5mg
- Price
- $158
- Updated
- 2024/03/01
- Product number
- 27977
- Product name
- GNE-477
- Packaging
- 10mg
- Price
- $299
- Updated
- 2024/03/01
- Product number
- CS-3359
- Product name
- GNE-477
- Purity
- 95.81%
- Packaging
- 10mg
- Price
- $320
- Updated
- 2021/12/16
GNE 477 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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