JZY3032 TFA
Based on 1 Customer Validation
JZY3032 (DALTAC-1) TFA is an orally active super inhibitor of androgen receptor (AR) and p300/CBP. JZY3032 TFA redirects the catalytic activity of p300 and locks the complex in a transcriptionally inactive state, thereby inhibiting AR-driven transcription and proliferation. JZY3032 TFA induces deep and durable tumor regression in castration-resistant and patient-derived xenograft models, and exhibits good tolerability. JZY3032 TFA can be used in research related to metastatic castration-resistant prostate cancer and prostate cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C54H63ClF5N13O4
- Molecular Weight:1088.61
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Speicherung:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
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p300 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| 22Rv1 | IC50 |
1.0 nM
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Inhibition of cell growth in AR-positive human 22Rv1 prostate cancer cells.
Inhibition of cell growth in AR-positive human 22Rv1 prostate cancer cells.
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d |
In Vitro
JZY3032 TFA (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].
JZY3032 TFA 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.
In Vivo
YZ3032 (60 mg/kg; p.o.) also achieves significant tumor inhibition in mice model, with good tolerance[1].
JZY3032 TFA 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.
- Research Protocol for Endocrine Diseases
- Patient-Derived Xenograft (PDX)
- Patient-Derived Orthotopic Xenograft (PDOX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Appearance Solid
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Molecular Weight 1088.61
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Formel C54H63ClF5N13O4
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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.OC(C(F)(F)F)=O
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Synonyms
DALTAC-1 TFA
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Reinheit & Dokumentation
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Data Sheet (284 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
JZY3032 TFA Related Classifications
HY-184124A Related Classifications
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Keywords
- JZY3032
- DALTAC-1
- JZY 3032
- JZY-3032
- DALTAC1
- DALTAC 1
- Androgen Receptor
- Histone Acetyltransferase
- HATs
- HAT
- patient-derived organoids
- HEK293 cells
- p300/CBP
- LNCaP
- metastatic castration-resistant prostate cancer
- AR-positive prostate cancer cells
- 22Rv1
- VCaP
- castration-resistant prostate cancer
- androgen receptor
- Inhibitor
- inhibitor
- inhibit