2. PROTAC Vitamin D Related/Nuclear Receptor Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. PROTACs Androgen Receptor Apoptosis PARP Caspase
  4. 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)).

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

BWA-6047

BWA-6047 Chemical Structure

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BWA-6047 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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

 

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 (ARW741L, ARF876L) 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.

BWA-6047 Related Antibodies

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 Cmax AUC F T1/2 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.
Molecular Weight

768.30

Formula

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
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
References
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BWA-6047 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:

BWA-6047BWA6047BWA 6047PROTACsAndrogen ReceptorApoptosisPARPCaspasepoly ADP ribose polymeraseandrogen receptornormal human liver epithelial cellsLNCaP xenograft tumorsCRBNprostate cancer cellsG1 to S phase transition 1androgen receptor splice variant 722Rv1 prostate cancer cellsenzalutamide-resistant cellsubiquitin-proteasome systemInhibitorinhibitorinhibit

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