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JZY3032

Katalog-Nr.GC81357 Copy One-Click Copy Product Info

JYZ3032 is an orally active super inhibitor of androgen receptor ( AR ) and p300/CBP.

Products are for research use only. Not for human use. We do not sell to patients.

JZY3032 Chemische Struktur

Größe Preis Lagerbestand Menge
1mg
540,00 $
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Sample solution is provided at 25 µL, 10mM.



Description of 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 [1].

In Vivo, JYZ3032 (30 mg/kg; i.p.) induces tumor regression in 75% of castrated male NSG mice bearing VCaP castration-resistant prostate cancer xenografts[1]. 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].

In Vitro, 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].

References:
[1]. Luo J, et al. Rewiring Oncogenic Transcriptional Complexes with Domain-ALTeration Chimeras (DALTACs) in Prostate Cancer[J]. bioRxiv, 2026: 2026.04. 24.720638.

Chemical Properties of JZY3032

Cas No. SDF
Formula C52H62ClF2N13O2 M.Wt 974.58
Löslichkeit DMSO: 100 mg/mL (102.61 mM; Need ultrasonic) Storage -20°C, protect from light, stored under argon
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of JZY3032

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1 mg 5 mg 10 mg
1 mM 1.0261 mL 5.1304 mL 10.2608 mL
5 mM 205.2 μL 1.0261 mL 2.0522 mL
10 mM 102.6 μL 513 μL 1.0261 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

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