2. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Androgen Receptor HSP CDK
  4. AR/AR-V7 degrader-1

AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer.

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AR/AR-V7 degrader-1

AR/AR-V7 degrader-1 Chemical Structure

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AR/AR-V7 degrader-1 Related Antibodies

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Description

AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer[1].

In Vitro

AR/AR-V7 degrader-1 (Compound 13) (0.25-2.5 μM) potently degrades AR and AR-V7 in 22Rv1 cells, achieving nearly complete degradation at the concentration of 2.5 μM[1].
AR/AR-V7 degrader-1 (0.01-5 μM; 0-48 h) mediates sustained, dose- and time-dependent degradation of AR and AR-V7 via the ubiquitin-proteasome pathway in 22Rv1 and VCaP cells, with DC50 values ranging from 0.6617 μM to 1.948 μM depending on the protein and cell line[1].
AR/AR-V7 degrader-1 potently inhibits the proliferation of 22Rv1 and VCaP cells, with IC50 values of 3.567 μM and 3.351 μM, respectively[1].
AR/AR-V7 degrader-1 (0-10 μM; 24 h) regulates the expression of cell cycle-related proteins (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest in 22Rv1 and VCaP cells[1].
AR/AR-V7 degrader-1 (0-2.5 μM; 0-24 h) downregulates the expression of AR/AR-V7 downstream biomarkers (PSA, TMPRSS2, FKBP51) in 22Rv1 and VCaP cells in a dose- and time-dependent manner[1].
AR/AR-V7 degrader-1 (1-2.5 μM; 24 h post-treatment) inhibits the migration of 22Rv1 and VCaP cells in a dose-dependent manner, and suppresses malignant colony formation and invasion of these cells[1].
AR/AR-V7 degrader-1 (5 μM; unspecified duration, in combination with 10 μM MG132) promotes the interaction between AR/AR-V7 and the E3 ubiquitin ligase HLTF, and inhibits the binding of AR/AR-V7 to HSP90 in 22Rv1 castration-resistant prostate cancer cells[1].

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

AR/AR-V7 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: 22Rv1 and VCaP CRPC cells
Concentration: 0, 0.01, 0.1, 0.5, 1, 2.5, 5 μM
Incubation Time: 0, 4, 8, 16, 24, 48 h
Result: Initiated degradation of AR and AR-V7 at approximately 0.5 μM in both cell lines.
Achieved DC50 values of 0.6617 μM for AR degradation and 0.852 μM for AR-V7 degradation in 22Rv1 cells.
Achieved DC50 values of 1.948 μM for AR degradation and 1.024 μM for AR-V7 degradation in VCaP cells.
Induced significant degradation of AR and AR-V7 within 8 h of treatment in both cell lines.

Cell Cycle Analysis[1]

Cell Line: 22Rv1 and VCaP CRPC cells
Concentration: 1-10 μM
Incubation Time: unspecified duration
Result: Markedly arrested both cell lines in the G0/G1 phase.

Western Blot Analysis[1]

Cell Line: 22Rv1 and VCaP CRPC cells
Concentration: 0, 0.5,1, 2.5μM
Incubation Time: 24 h
Result: Significantly downregulated expression of CDK4, CDK6, Cyclin D1, and Cyclin E1.
Significantly upregulated expression of P21 in both cell lines.\nDownregulated expression of PSA, TMPRSS2, and FKBP51 in both cell lines in a dose-dependent manner.
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ T1/2 Tmax Cmax Bioavailability
Mice[1] 30 mg/kg p.o. 13433.63 ng·h/mL 16106.59 ng·h/mL 7.88 h 12.76 h 9.23 h 1.00 h 1162.86 ng/mL 24.70 %
Mice[1] 10 mg/kg i.v. 18137.97 ng·h/mL 20709.35 ng·h/mL 6.43 h 10.18 h 8.63 h 0.083 h 5074.99 ng/mL /
In Vivo

AR/AR-V7 degrader-1 (30-60 mg/kg; p.o.; daily; 14 days/single dose) potently inhibits the growth of 22Rv1 castration-resistant prostate cancer (CRPC) tumors in Balb/c nude mice and induces the degradation of AR and AR-V7 in tumor tissues[1].

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

Animal Model: Balb/c nude (male)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; daily; 14 days/single dose
Result: Significantly reduced tumor volume and tumor weight relative to vehicle control.
Produced greater tumor growth inhibition at 60 mg/kg than 30 mg/kg.
Markedly suppressed expression of AR, AR-V7, and their downstream biomarkers (PSA, FKBP51, TMPRSS2) at 60 mg/kg.
Reduced AR and Ki67 expression in tumor tissues.
Caused no significant changes in mouse body weight, indicating favorable tolerability.
Induced AR and AR-V7 degradation in tumor tissues as early as 6 hours post-administration.
Sustained suppression of both proteins through 48 hours.
Showed no significant recovery of AR/AR-V7 expression until 72 hours post-dose.
Molecular Weight

678.80

Formula

C33H33F3N6O3SSi
SMILES

S=C(N(C1=CC(C(F)(F)F)=C(C#N)C=C1)C(C2(C)C)=O)N2C3=CC=C(OCCN4C=C(CCO[Si](C)(C5=CC=CC=C5)C)N=N4)C=C3
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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AR/AR-V7 degrader-1 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:

AR/AR-V7 degrader-1Androgen ReceptorHSPCDKHeat shock proteinsCyclin dependent kinaseAR and AR-V7 degradercastration-resistant prostate cancer22Rv1 cellsVCaP cellsBalb/c nude mice
Inhibitorinhibitorinhibit

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