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Art. -Nr.: HY-175541

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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)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2926610-43-5
Formel: C₄₀H₄₇N₁₁O₅
Molecular Weight:761.87

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

TQ-3959 Chemical Structure

CAS. Nr.: 2926610-43-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: Btk ligand (HY-175543); Blue: Cereblon ligand (HY-W733888); Black: linker (HY-W061884)).

IC₅₀ & Target^[1]

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

TQ-3959 exhibits potent BTK degradation activity with a DC₅₀ of 0.4 nM and a D_max 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.

Parmacokinetics

Species	Dose	Route	AUC_0-∞	T_1/2	C_max	V_d	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 %

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.

Chemical Information

CAS. Nr. 2926610-43-5
Molecular Weight 761.87
Formel C₄₀H₄₇N₁₁O₅
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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TQ-3959

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

TQ-3959 Related Classifications

HY-175541 Related Classifications