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Art. -Nr.: HY-176128

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BWA-6047

BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC₅₀ values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer.
(Pink: Androgen Receptor ligand (HY-176129); Blue: Cereblon ligand (HY-W069604); Black: linker (HY-B0236)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₄₂H₄₆ClN₅O₇
Molecular Weight:768.30

Speicherung:

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

Data Sheet (274 KB)

BWA-6047 Chemical Structure

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

Biologische Aktivität

Beschreibung

BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC₅₀ values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer^[1]. (Pink: Androgen Receptor ligand (HY-176129); Blue: Cereblon ligand (HY-W069604); Black: linker (HY-B0236)).

IC₅₀ & Target^[1]

Cereblon

PARP-1

Caspase 3

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle PARP Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

In Vitro

BWA-6047 (0.01-300 μM; 2-36 h) dose- and time-dependently degrades AR, AR-V7, and GSPT1 in LNCaP, VCaP, and 22Rv1 prostate cancer cells via a CRBN- and proteasome-dependent mechanism (DC₅₀ = 0.6-15.6 nM), with potent activity even in Enzalutamide (HY-70002)-resistant cells^[1].
BWA-6047 (0.01-1000000 nM; 72 h) potently inhibits the proliferation of AR-dependent prostate cancer cells, including Enzalutamide-resistant lines, with low activity against AR-independent cancer cells and normal cells^[1].
BWA-6047 (0.01-100000 nM; 24 h) potently inhibits the transcriptional activity of wild-type and Enzalutamide-resistant AR mutants (AR^W741L, AR^F876L) in 293T cells^[1].
BWA-6047 (1-100 nM; 24 h) suppresses the expression of AR downstream target genes (PSA, TMPRSS2, FKBP5) in 22Rv1 and LNCaP prostate cancer cells^[1].
BWA-6047 (1-30 nM; 24 h) induces G1 phase cell cycle arrest in 22Rv1 prostate cancer cells in a dose-dependent manner^[1].
BWA-6047 (1-100 nM; 24 h) induces apoptosis in 22Rv1 and LNCaP prostate cancer cells, as evidenced by increased levels of cleaved apoptotic markers^[1].
BWA-6047 (30 nM; 12 h) promotes the polyubiquitination of AR and GSPT1 in 22Rv1 prostate cancer cells, a key step in proteasomal degradation^[1].

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

Real Time qPCR^[1]

Cell Line:

22Rv1 and LNCaP prostate cancer cells
Concentration:

1, 3 nM (22Rv1 cells); 10, 30, 100 nM (LNCaP cells)
Incubation Time:

24 h
Result:

Significantly decreased mRNA levels of PSA, TMPRSS2, and FKBP5 at 1 nM and 3 nM in 22Rv1 cells.
Significantly decreased mRNA levels of PSA, TMPRSS2, and FKBP5 at 10 nM, 30 nM, and 100 nM in LNCaP cells.

Cell Cycle Analysis^[1]

Cell Line:

22Rv1 prostate cancer cells
Concentration:

1, 3, 10, 30 nM
Incubation Time:

24 h
Result:

Increased G1 phase proportion from 49.7% (control) to 56.3% (1 nM), 55.6% (3 nM), 58.9% (10 nM), and 74.6% (30 nM) in 22Rv1 cells.
Decreased corresponding S phase proportion from 41.4% to 34.1%, 36.6%, 33.4%, and 22.3% in 22Rv1 cells.

Western Blot Analysis^[1]

Cell Line:

22Rv1 and LNCaP prostate cancer cells
Concentration:

1, 3, 10, 30 μM (22Rv1 cells); 1, 3, 10, 30, 100 μM (LNCaP cells)
Incubation Time:

24 h
Result:

Induced dose-dependent increases in cleaved-PARP-1 and cleaved-caspase-3 levels in 22Rv1 cells.
Induced dose-dependent increases in cleaved-PARP-1 and cleaved-caspase-3 levels in LNCaP cells.

Parmacokinetics

Species	Dose	Route	C_max	AUC	F	T_1/2	CL
Mice^[1]	2 mg/kg	i.v.	1121 ng/mL	1850 ng·h/mL	/	0.9 h	1081 mL/h/kg
Mice^[1]	10 mg/kg	p.o.	206 ng/mL	1035 ng·h/mL	11.2 %	/	/

In Vivo

BWA-6047 (20 mg/kg; p.o.; daily; 26 days) achieves 60.0% tumor growth inhibition in castrated male NOD SCID mice bearing LNCaP xenografts, with significant reductions in intratumoral AR, GSPT1, and serum PSA, and no apparent toxicity^[1].

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

Animal Model:

NOD SCID mice bearing LNCaP xenografts (male, 6 weeks old, castrated after tumor reached ~180 mm³)^[1]
Dosage:

20 mg/kg
Administration:

p.o.; daily; 26 days
Result:

Achieved 60.0% tumor growth inhibition (TGI) relative to the vehicle control.
Significantly reduced intratumoral levels of androgen receptor (AR) and G1 to S phase transition 1 (GSPT1) proteins compared to the vehicle control.
Significantly reduced serum prostate-specific antigen (PSA) concentrations compared to the vehicle control.
Showed no observable weight loss in treated mice.

Chemical Information

Molecular Weight 768.30
Formel C₄₂H₄₆ClN₅O₇
SMILES

O=C(CCCCCNC1=CC=C2C(N(C3C(NC(CC3)=O)=O)C(C2=C1)=O)=O)N4CCC(CC4)COC5=C(C#N)C=C(C(C)(C6=CC=C(C=C6)OC)C)C=C5Cl
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]. Zhang B, et al. Rational Design of Dual Degraders by Incorporating Molecular Glue Structural Features into PROTAC Degraders. J Med Chem. 2025;68(10):10268-10298. [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.

100 mg

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

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BWA-6047

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle PARP Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

BWA-6047 Related Classifications

HY-176128 Related Classifications