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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C52H62ClF2N13O2
- 分子量:974.58
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保管条件:
-20°C, protect from light, stored under argon
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under argon)
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
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p300 |
体外実験
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).
Parmacokinetics
体内実験
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.
化学情報
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性状 Solid
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分子量 974.58
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分子式 C52H62ClF2N13O2
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Color White to light yellow
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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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under argon
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under argon)
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (102.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under argon). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under argon). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (252 KB)
- English - EN (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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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under argon). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.0261 mL | 5.1304 mL | 10.2608 mL | 25.6521 mL |
| 5 mM | 0.2052 mL | 1.0261 mL | 2.0522 mL | 5.1304 mL | |
| 10 mM | 0.1026 mL | 0.5130 mL | 1.0261 mL | 2.5652 mL | |
| 15 mM | 0.0684 mL | 0.3420 mL | 0.6841 mL | 1.7101 mL | |
| 20 mM | 0.0513 mL | 0.2565 mL | 0.5130 mL | 1.2826 mL | |
| 25 mM | 0.0410 mL | 0.2052 mL | 0.4104 mL | 1.0261 mL | |
| 30 mM | 0.0342 mL | 0.1710 mL | 0.3420 mL | 0.8551 mL | |
| 40 mM | 0.0257 mL | 0.1283 mL | 0.2565 mL | 0.6413 mL | |
| 50 mM | 0.0205 mL | 0.1026 mL | 0.2052 mL | 0.5130 mL | |
| 60 mM | 0.0171 mL | 0.0855 mL | 0.1710 mL | 0.4275 mL | |
| 80 mM | 0.0128 mL | 0.0641 mL | 0.1283 mL | 0.3207 mL | |
| 100 mM | 0.0103 mL | 0.0513 mL | 0.1026 mL | 0.2565 mL |
JZY3032 関連分類
HY-184124 関連分類
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