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-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545) ) [1].

Product Specifications

CAS Number

[2926610-43-5]

UNSPSC

12352005

Target

Btk; PROTACs

Related Pathways

PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

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

Molecular Formula

C40H47N11O5

Molecular Weight

761.87

References & Citations

[1]Ren J, et al. Discovery of TQ-3959 as a Potent and Orally Bioavailable BTK PROTAC Degrader Incorporating a Novel Benzisoxazole-Based CRBN Ligand for the Treatment of B-Cell Malignancies. J Med Chem. 2025 Aug 14;68 (15) :15960-15979.