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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| 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. |
| Molecular Weight | 761.87 |
| Formula | C40H47N11O5 |
| Cas No. | 2926610-43-5 |
| Smiles | O=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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
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
and mix thoroughly until a homogeneous solution is obtained.
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