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GNE-477

Cat. No. M6226
GNE-477 Structure
Size Price Availability Quantity
5mg USD 400 In stock
10mg USD 650 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: GNE-477 (Compound 8) has improved potency in the MCF7.1 cell proliferation assay with an EC50 of 143 nM.

In vivo: GNE-477 also exhibits stasis in a PC3 tumor growth inhibition study. In an experiment evaluating the tumor growth inhibition of a PC3 tumor xenograft over 14 days, stasis is achieved at a 20 mg/kg QD dose and significant inhibition is observed with doses as low as 1 mg/kg QD. GNE-477 is generally well tolerated during this study as demonstrated by acceptable levels of weight loss comparable to that observed with the animals in the vehicle cohort.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Rats
Formulation 0.5% methylcellulose/0.2% Tween-80
Dosages 1 mg/kg
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 504.63
Formula C21H28N8O3S2
CAS Number 1032754-81-6
Purity >98%
Solubility 9.2 mg/mL in DMSO
Storage at -20°C
References

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Heffron TP, et al. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11. PMID: 20346656.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GNE-477 supplier, mTOR, inhibitors

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