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Cat. No.: HY-175541

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TQ-3959

Name: TQ-3959
Brand: MedChemExpress
SKU: HY-175541
Price: 780.00 USD
Availability: InStock
Rating: 5 (1 reviews)

TQ-3959 is an orally active BTK PROTAC degrader with a DC₅₀ of 0.4 nM. TQ-3959 selectively and efficiently degrades BTK by recruiting the CRBN E3 ubiquitin ligase and utilizing the ubiquitin-proteasome system. TQ-3959 can be applied in the research of B-cell malignancies and lymphomas.
(Pink: Btk ligand (HY-175543); Blue: Cereblon ligand (HY-W733888); Black: linker (HY-W061884)).

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

CAS No.: 2926610-43-5
Formula: C₄₀H₄₇N₁₁O₅
Molecular Weight:761.87

Storage:

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

Data Sheet (285 KB)

TQ-3959 Chemical Structure

CAS No.: 2926610-43-5

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

TQ-3959 is an orally active BTK PROTAC degrader with a DC₅₀ of 0.4 nM. TQ-3959 selectively and efficiently degrades BTK by recruiting the CRBN E3 ubiquitin ligase and utilizing the ubiquitin-proteasome system. TQ-3959 can be applied in the research of B-cell malignancies and lymphomas^[1]. (Pink: Btk ligand (HY-175543); Blue: Cereblon ligand (HY-W733888); Black: linker (HY-W061884)).

IC₅₀ & Target

^[1]

Cereblon

All PROTACs Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC50	>1000 nM	Cell proliferation inhibition against human HEK293 cells assessed by CCK-8 assay. Cell proliferation inhibition against human HEK293 cells assessed by CCK-8 assay.	40731261
HUVEC	IC50	>1000 nM	Cell proliferation inhibition against human HUVEC cells assessed by CCK-8 assay. Cell proliferation inhibition against human HUVEC cells assessed by CCK-8 assay.	40731261
OCI-Ly10	DC₅₀	0.4 nM	BTK protein degradation in human OCI-Ly10 lymphoma cells incubated for 6 hrs via HTRF assay. BTK protein degradation in human OCI-Ly10 lymphoma cells incubated for 6 hrs via HTRF assay.	40731261
OCI-Ly10	IC₅₀	0.08 nM	Antiproliferative activity against human OCI-Ly10 (BTK^WT) lymphoma cells incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human OCI-Ly10 (BTK^WT) lymphoma cells incubated for 72 hrs by CCK-8 assay.	40731261
TMD8	IC₅₀	1.0 nM	Antiproliferative activity against human TMD-8 (BTK^WT) lymphoma cells incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human TMD-8 (BTK^WT) lymphoma cells incubated for 72 hrs by CCK-8 assay.	40731261
OCI-Ly10	IC₅₀	0.2 nM	Antiproliferative activity against human OCI-Ly10 (BTK^C481S) lymphoma cells incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human OCI-Ly10 (BTK^C481S) lymphoma cells incubated for 72 hrs by CCK-8 assay.	40731261
TMD8	IC₅₀	0.6 nM	Antiproliferative activity against human TMD-8 (BTK^C481S) lymphoma cells incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human TMD-8 (BTK^C481S) lymphoma cells incubated for 72 hrs by CCK-8 assay.	40731261

In Vitro

TQ-3959 (9.8 pM-10 nM; 6 h) potently degrades BTK in OCI-Ly10 lymphoma cells, with a DC₅₀ of 0.4 nM and a maximum degradation rate of 97.7%^[1].
TQ-3959 (0.06 nM-5 μM; 72 h) potently inhibits the proliferation of OCI-Ly10 BTK^WT, TMD-8 BTK^WT, OCI-Ly10 BTK^C481S and TMD-8 BTK^C481S lymphoma cells, with IC₅₀ values of 0.08, 1.0, 0.2 and 0.6 nM, respectively, but exhibits extremely low antiproliferative activity against normal HEK293 and HUVEC cells, with IC₅₀ values >1 μM^[1].
TQ-3959 (starting at 1 μM, 7 concentration gradients with 4-fold dilution; 2.5 h) potently inhibits BTK^WT (IC₅₀ = 12.3 nM) and BTK^C481S (IC₅₀ = 26.2 nM), and exhibits high selectivity over EGFR (the IC₅₀ of EGFR is 512-fold higher)^[1].

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

Parmacokinetics

Species	Dose	Route	V_d	CL	AUC_0-∞	T_1/2	C_max	F
Mice^[1]	1 mg/kg	i.v.	0.4 L/kg	0.2 L/h/kg	/	/	/	/
Mice^[1]	10 mg/kg	p.o.	/	/	35778 ng·h/mL	2.9 h	3848 ng/mL	58.0 %

In Vivo

TQ-3959 (7.5-30 mg/kg; p.o.; once daily; for 20 consecutive days) potently inhibits the growth of TMD-8 tumors in NOD-SCID mice and achieves complete tumor regression^[1].

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

Animal Model:

NOD-SCID (female, 6-8 weeks old) were subcutaneously implanted into the right flank with 1 x 10⁶ TMD-8 cells^[1]
Dosage:

7.5 mg/kg, 15 mg/kg, 30 mg/kg
Administration:

p.o.; once daily; 20 days
Result:

Achieved a tumor growth inhibition (TGI) rate of 80.5% and a mean tumor weight of 0.253 g at 7.5 mg/kg.
Achieved a TGI rate of 98.5%, a mean tumor weight of 0.019 g, and 1 complete tumor regression at 15 mg/kg.
Achieved a TGI rate of 98.8%, a mean tumor weight of 0.016 g, and 2 complete tumor regressions at 30 mg/kg.
Induced minimal animal weight loss during the study.

Chemical Information

CAS No. 2926610-43-5
Molecular Weight 761.87
Formula 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 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)

References

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

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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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100 mg

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