TQ-3959
TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.
(Pink: Btk ligand (HY-175543); Blue: Cereblon ligand (HY-W733888); Black: linker (HY-W061884)).
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- CAS No.: 2926610-43-5
- Formule: C40H47N11O5
- Masse moléculaire:761.87
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Cereblon |
TQ-3959 exhibits potent BTK degradation activity with a DC50 of 0.4 nM and a Dmax of 97.7% in OCI-Ly10 cells via HTRF assay[1].
TQ-3959 (72 h) shows 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)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-∞ | T1/2 | Cmax | Vd | CL | F |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 35778 ng·h/mL | 2.9 h | 3848 ng/mL | 0.4 L/kg | 0.0002 mL/h/kg | 58 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:TMD-8 cells (1 × 107 in 100 μL) were subcutaneously implanted into the right flanks of 6-8-week-old female NOD-SCID mice[1]
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Dosage:7.5, 15, 30 mg/kg
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Administration:p.o. once daily for 20 days
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Result:Achieved tumor growth inhibition (TGI) rates of 80.5%, 98.5%, and 98.8% at oral doses of 7.5, 15, and 30 mg/kg in female NOD-SCID mice bearing TMD-8 xenografts, respectively.
Showed no significant changes in body weight.
Chemical Information
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CAS No. 2926610-43-5
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Masse moléculaire 761.87
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Formule C40H47N11O5
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SMILES
NC(C1=C(NC2=CC=C(C3CCN(CC3)C4CN(C5=CC6=C(C=C5)C(C7CCC(NC7=O)=O)=NO6)C4)C=C2)N=C(N8C[C@H](N9CCN(C)C9=O)CCC8)C=N1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TQ-3959 Related Classifications
HY-175541 Related Classifications
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