Cat. No.: HY-11042

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GNE-477

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

GNE-477 is a potent and efficacious dual PI3K (IC₅₀=4 nM)/mTOR(K_i=21 nM) inhibitor.

For research use only. We do not sell to patients.

Purity: 98.75%
CAS No.: 1032754-81-6
Formula: C₂₁H₂₈N₈O₃S₂
Molecular Weight:504.63

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GNE-477 Chemical Structure

CAS No.: 1032754-81-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

GNE-477 is a potent and efficacious dual PI3K (IC₅₀=4 nM)/mTOR(K_i=21 nM) inhibitor.

IC₅₀ & Target^[1]

PI3Kα

4 nM (IC₅₀)

mTOR

21 nM (Ki)

All PI3K Isoforms :

All mTOR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	EC₅₀	174 nM Compound: 8, GNE-477	Antiproliferative activity against human PC3 cells after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human PC3 cells after 3 days by celltiter-glo luminescence assay	[PMID: 20346656]
PC-3	IC₅₀	220 nM Compound: 4	Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay	[PMID: 21981714]

In Vitro

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1032754-81-6
Appearance Solid
Molecular Weight 504.63
Formula C₂₁H₂₈N₈O₃S₂
Color Light yellow to yellow
SMILES

NC1=NC=C(C2=NC(N3CCOCC3)=C4C(C(C)=C(CN5CCN(S(=O)(C)=O)CC5)S4)=N2)C=N1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11;11:580407. PMID: 33343350

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL (33.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9816 mL

9.9082 mL

19.8165 mL

5 mM

0.3963 mL

1.9816 mL

3.9633 mL

10 mM

0.1982 mL

0.9908 mL

1.9816 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.67 mg/mL (3.31 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.67 mg/mL (3.31 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Animal Administration^[1]

Mice, Rats and Dogs^[1]
Female nu/nu mice are dosed with the GNE-477 HCl salt as a solution intraveinously (1 mg/kg) in 5% DMSO/5% cremophor and dosed orally as a solution in 80% PEG (5 mg/kg). Male rats are dosed with the GNE-477 TFA salt as a solution intraveinously (1 mg/kg) in 5% DMSO/5% cremophor and dosed orally as a solution in 80% PEG (5 mg/kg). Male beagle dogs are dosed with the GNE-477 HCl salt as a solution intraveinously (1 mg/kg) in 10% HP-β-CD and dosed orally as a suspension in MCT (2 mg/kg). Efficacy study of GNE-477 in the PC3-NCI tumor xenograft model is proformed. The percent of tumor growth inhibition (TGI) at the end of study (day 14) is measured and compared with the vehicle control group.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9816 mL	9.9082 mL	19.8165 mL	49.5412 mL
	5 mM	0.3963 mL	1.9816 mL	3.9633 mL	9.9082 mL
	10 mM	0.1982 mL	0.9908 mL	1.9816 mL	4.9541 mL
	15 mM	0.1321 mL	0.6605 mL	1.3211 mL	3.3027 mL
	20 mM	0.0991 mL	0.4954 mL	0.9908 mL	2.4771 mL
	25 mM	0.0793 mL	0.3963 mL	0.7927 mL	1.9816 mL
	30 mM	0.0661 mL	0.3303 mL	0.6605 mL	1.6514 mL

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GNE-477

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

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Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) GNE-477

All PI3K Isoforms

All mTOR Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GNE-477 Related Classifications

HY-11042 Related Classifications