2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Btk
  4. 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)).

For research use only. We do not sell to patients.

TQ-3959

TQ-3959 Chemical Structure

CAS No. : 2926610-43-5

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TQ-3959 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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].

IC50 & Target[1]

Cereblon

 

In Vitro

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.

TQ-3959 Related Antibodies
In Vivo

TQ-3959 (7.5-30 mg/kg, p.o., once daily, 20 days) exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 7.5, 15, 30 mg/kg
Administration: p.o. once daily for 20 days
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.
Molecular Weight

761.87

Formula

C40H47N11O5
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TQ-3959 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TQ-39592926610-43-5TQ3959TQ 3959PROTACsBtkBruton tyrosine kinasechronic lymphocytic leukemia (CLL)MT-802BTKPROTACInhibitorinhibitorinhibit

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