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
- Molecular Weight:
- 504.63
- MDL Number:
- MFCD20527726
- MOL File:
- 1032754-81-6.mol
- MSDS File:
- SDS
| 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) |
| FDA UNII | 0E8LA9H0RY |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H317-H319 |
| Precautionary statements | P280-P305+P351+P338 |
GNE 477 price More Price(20)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 27977 | GNE-477 | 1032754-81-6 | 25mg | $667 | 2024-03-01 | Buy |
| Cayman Chemical | 27977 | GNE-477 | 1032754-81-6 | 50mg | $1018 | 2024-03-01 | Buy |
| Cayman Chemical | 27977 | GNE-477 | 1032754-81-6 | 5mg | $158 | 2024-03-01 | Buy |
| Cayman Chemical | 27977 | GNE-477 | 1032754-81-6 | 10mg | $299 | 2024-03-01 | Buy |
| ChemScene | CS-3359 | GNE-477 95.81% | 1032754-81-6 | 10mg | $320 | 2021-12-16 | Buy |
GNE 477 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7553 | 61 |
| SYN|thesis med chem P/L | +86-021-50720296 | service@synkinase.com | China | 266 | 58 |
| AdooQ BioScience, LLC | +1 (866) 930-6790 | info@adooq.com | United States | 2784 | 58 |