ChemicalBook > CAS DataBase List > GNE 477

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
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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
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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.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
27977
Product name
GNE-477
Packaging
25mg
Price
$667
Updated
2024/03/01
Cayman Chemical
Product number
27977
Product name
GNE-477
Packaging
50mg
Price
$1018
Updated
2024/03/01
Cayman Chemical
Product number
27977
Product name
GNE-477
Packaging
5mg
Price
$158
Updated
2024/03/01
Cayman Chemical
Product number
27977
Product name
GNE-477
Packaging
10mg
Price
$299
Updated
2024/03/01
ChemScene
Product number
CS-3359
Product name
GNE-477
Purity
95.81%
Packaging
10mg
Price
$320
Updated
2021/12/16
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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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GNE 477 Suppliers

China 51 France 1 United Kingdom 1 United States 12 Global 65
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7553
Advantage
61
SYN|thesis med chem P/L
Tel
+86-021-50720296
Fax
+86-021-50720297
Email
service@synkinase.com
Country
China
ProdList
266
Advantage
58
AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
Email
info@adooq.com
Country
United States
ProdList
2784
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3466
Advantage
58
Sichuan Wei Keqi Biological Technology Co., Ltd.
Tel
028-81700200 18116577057
Fax
028-81705658
Email
3003855609@qq.com
Country
China
ProdList
7887
Advantage
56
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2991
Advantage
60
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4335
Advantage
55
Guangzhou Zhiya Chemdrugs Co.,Ltd
Tel
18122150900
Fax
QQ:2869377561
Email
sculk28@163.com
Country
China
ProdList
646
Advantage
55
SPIRO PHARMA
Tel
Fax
-
Email
eric_feng1954@126.com
Country
China
ProdList
9254
Advantage
55

1032754-81-6, GNE 477Related Search:

GNE-3511 GNE-490 GNE-9605 GNE-6640 GNF 5837 GNE-955 GNE140 GNE-493 gne-131 GNE 617 GNE 7915

  • 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
  • 1032754-81-6
  • C21H28N8O3S2