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TQ-3959

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Catalog No. T212293Cas No. 2926610-43-5

TQ-3959 is an orally active BTKPROTAC degrader, with a DC50 of 14.6 nM. It exhibits antiproliferative activity against both wild-type BTK and BTK C481S mutant cell lines. TQ-3959 demonstrates tumor growth inhibition in female NOD-SCID mice with TMD-8 xenografts. This compound is applicable in the study of B-cell malignancies, such as lymphoma.

TQ-3959

TQ-3959

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Catalog No. T212293Cas No. 2926610-43-5
TQ-3959 is an orally active BTKPROTAC degrader, with a DC50 of 14.6 nM. It exhibits antiproliferative activity against both wild-type BTK and BTK C481S mutant cell lines. TQ-3959 demonstrates tumor growth inhibition in female NOD-SCID mice with TMD-8 xenografts. This compound is applicable in the study of B-cell malignancies, such as lymphoma.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mgInquiry10-14 weeks10-14 weeks
50 mgInquiry10-14 weeks10-14 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction

Bioactivity
Description
TQ-3959 is an orally active BTKPROTAC degrader, with a DC50 of 14.6 nM. It exhibits antiproliferative activity against both wild-type BTK and BTK C481S mutant cell lines. TQ-3959 demonstrates tumor growth inhibition in female NOD-SCID mice with TMD-8 xenografts. This compound is applicable in the study of B-cell malignancies, such as lymphoma.
In vitro
TQ-3959 demonstrates potent BTK degradation activity in OCI-Ly10 cells through HTRF experiments, with a DC₅₀ of 0.4 nM and a Dmax of 97.7%. Over 72 hours, TQ-3959 exhibits antiproliferative activity against OCI-Ly10 (BTK WT cells) (IC₅₀ = 0.08 nM), TMD-8 (BTK WT cells) (IC₅₀ = 1.0 nM), OCI-Ly10 (BTK C481S cells) (IC₅₀ = 0.2 nM), and TMD-8 (BTK C481S cells) (IC₅₀ = 0.6 nM).
In vivo
TQ-3959, administered orally at doses of 7.5-30 mg/kg once daily for 20 days, has been shown to inhibit tumor growth in NOD-SCID mice xenografted with TMD-8.
Chemical Properties
Molecular Weight761.87
FormulaC40H47N11O5
Cas No.2926610-43-5
SmilesO=C1C(C=2C=3C(=CC(=CC3)N4CC(C4)N5CCC(CC5)C6=CC=C(NC7=NC(=CN=C7C(N)=O)N8C[C@@H](CCC8)N9C(=O)N(C)CC9)C=C6)ON2)CCC(=O)N1
Storage & Solubility Information
StoragePowder: -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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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
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