JZY3032
JYZ3032 is an orally active super inhibitor of androgen receptor (AR) and p300/CBP. JYZ3032 redirects the catalytic activity of p300 and locks the complex in a transcriptionally inactive state, thereby inhibiting AR-driven transcription and proliferation. JYZ3032 induces deep and durable tumor regression in castration-resistant and patient-derived xenograft models, and exhibits good tolerability. JYZ3032 can be used in research related to metastatic castration-resistant prostate cancer and prostate cancer.
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- Formule: C52H62ClF2N13O2
- Masse moléculaire:974.58
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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p300 |
JYZ3032 (1.0 nM; 120 h) potently inhibits the growth of 22Rv1 prostate cancer cells with an IC50 of 1.0 nM and 69% maximum growth inhibition[1].
JYZ3032 (100 nM, Serial dilutions; 4 h pulse treatment, total 120 h) exhibits durable, sustained growth inhibitory activity in VCaP and LNCaP prostate cancer cells, with a 4-hour pulse treatment yielding comparable efficacy to continuous exposure[1].
JYZ3032 potently suppresses enhancer-associated histone acetylation marks in VCaP prostate cancer cells but not in AR-negative Kelly neuroblastoma cells, demonstrating lineage selectivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:22Rv1 prostate cancer cells
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Concentration:1.0 nM
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Incubation Time:120 h
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Result:Inhibited 22Rv1 cell growth with an IC50 of 1.0 nM and a maximum inhibition (Imax) of 69%.
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Cell Line:VCaP, LNCaP, CWR-R1 prostate cancer cells
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Concentration:Serial dilutions
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Incubation Time:120 h
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Result:Exhibited potent cytotoxicity across all tested AR-positive prostate cancer cells, with superior activity relative to the combined treatment with AR-LBD inhibitor JZY3221 and p300/CBP BRD inhibitor GNE-049.
Activity was comparable to or better than the p300/CBP dual degrader CBPD-409 (HY-158113).
YZ3032 (60 mg/kg; p.o.) also achieves significant tumor inhibition with good tolerance[1].
JYZ3032 induces complete tumor regression and 100% survival for at least 35 days in NSG mice bearing patient-derived prostate cancer xenografts of MDA-PCa-183, significantly inhibits tumor growth in the MDA-PCa-146-12 model, and exhibits good tolerance[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG (male, castrated)[1]
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Dosage:30 mg/kg (i.p.); 60 mg/kg (p.o.)
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Administration:i.p.; p.o.
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Result:Induced tumor regression in 75% (12 of 16) of treated tumors.
Achieved robust tumor suppression that outperformed a combination of a p300 bromodomain inhibitor and an AR-LBD inhibitor.
Increased AR-p300 proximity in treated tumors.
Reduced ERG, PSA, MYC, Ki67, H3K27ac, and H2BK20ac signals in treated tumors.
Left AR, p300, and CBP levels unchanged.
Caused no significant changes in body weight, serum liver/kidney function, or hematologic parameters.
Chemical Information
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Masse moléculaire 974.58
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Formule C52H62ClF2N13O2
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SMILES
CN1N=CC(C2=CC3=C(N(C4=NN([C@H](CC5)CC[C@@H]5CN(CC6)CCN6C(C=C7)=NN=C7C(N[C@H]8CC[C@@H](CC8)N(C)C9=CC=C(C(Cl)=C9)C#N)=O)C%10=C4CN(C(C)=O)CC%10)CCC3)C=C2C(F)F)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JZY3032 Related Classifications
HY-184124 Related Classifications
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