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NEO-811

Name: NEO-811
Brand: TargetMol
SKU: T217535
Rating: 4.5 (1 reviews)

Catalog No. T217535 Copy Product Info

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NEO-811 is a potent, selective, and cereblon (CRBN)-dependent E3 ubiquitin ligase-mediated proteolytic inhibitor that targets ARNT (HIF-1β). NEO-811 blocks the ccRCC signaling pathway by degrading ARNT, thereby inhibiting the survival and proliferation of tumor cells. NEO-811 is suitable for use in studies of clear cell renal cell carcinoma (ccRCC).

NEO-811

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Catalog No. T217535

NEO-811

Cas No. 3084635-77-5

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Product Introduction

Bioactivity

Description

In vivo

In clear cell renal cell carcinoma (ccRCC) xenograft models (containing the HIF-2α G323E resistance mutation) and patient-derived xenograft (PDX) models, in vivo administration of NEO-811 as a single agent induced regression of ccRCC tumors and remained effective in G323E mutant models resistant to HIF-2α antagonists; In PDX models, its antitumor activity was superior to that of clinically available HIF-2 antagonists and VEGFR tyrosine kinase inhibitors. [1]

Chemical Properties

Molecular Weight	543.59
Formula	C₃₀H₃₀FN₅O₄
Cas No.	3084635-77-5
Smiles	O[C@]1(C(C)(C)CN(CC2=CC=C(C=C2)C=3N=CON3)CC1)C4=C(F)C5=C(C=C4)N=CC(=C5)C6C(=O)NC(=O)CC6

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc