GNE 477
- CAS NO.:1032754-81-6
- Empirical Formula: C21H28N8O3S2
- Molecular Weight: 504.63
- MDL number: MFCD20527726
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:13
What is GNE 477?
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].
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.
Properties of GNE 477
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 |
Safety information for GNE 477
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H317:Sensitisation, Skin H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for GNE 477
New Products
Tubulysin H Tubulysin B Tubulysin E (R)-tert-butyl (4-methyl-1-oxopentan-3-yl)carbamate 2-(azetidin-3-ylidene)acetonitrile (hydrochloride) 3-Aminocyclobutanone hydrochloride 4-(Benzyloxy)-3-bromophenylacetic Acid 1,2,3,6-TETRAHYDROPYRIDINE HYDROCHLORIDE 1-(1,1-Difluoroethyl)-2-fluorobenzene CYCLOBUTYLAMINE HYDROCHLORIDE 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate Fuel shell Calcium Sodium Phosphosilicate IH 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine Imeglimin Hydrochloride IH Lubiprostone Latanoprostene Bunod Magnesium Trisilicate Flame Retardant Zinc Borate methyl 3-fluoro-4- thiomorpholino phenylcarbamate (R)-(3-(3-fluoro-4- thiomorpholinophenyl)-2- oxooxazolidin-4-yl) methyl methanesulfonate 1H-Imidazole-4-carbonitrile 7-Methoxyquinoline-4-carboxylic acidRelated products of tetrahydrofuran
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