AZ'3137
Based on 1 Customer Validation
AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC50 value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC50 of 92 nM). AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice.
(Pink: Androgen Receptor ligand (HY-172954); Blue: Cereblon ligand (HY-172955); Black: linker (HY-W262798)).
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。
- 純度: 99.90%
- CAS 番号: 2960179-55-7
- 分子式: C43H47F4N7O4
- 分子量:801.87
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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Anti-Cancer Compound Library
HY-L025
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Orally Active Compound Library
HY-L061
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Transcription Factor-Targeted Library
HY-L090
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Anti-Prostate Cancer Compound Library
HY-L124
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Nuclear Receptor Compound Library
HY-L126
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PROTAC Library
HY-L151
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | GI50 |
74 nM
Compound: 22; AZ'3137
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Anti-proliferative activity against human LNCaP cells assessed as number of live cells measured after 7 days by Sytox Green Nucleic Acid stain assay
Anti-proliferative activity against human LNCaP cells assessed as number of live cells measured after 7 days by Sytox Green Nucleic Acid stain assay
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[PMID: 38991141] |
AZ'3137 (Compound 22; 0-10 μM; 7 days) can inhibit AR signaling and cell proliferation of prostate cancer cell line LNCaP[1].
AZ′3137 (0.1 nM-10 μM; 24 h) inhibits the expression of AR target genes in LNCaP cells[1].
AZ′3137 (0.1 nM-10 μM; 24 h) is able to degrade AR in C4-2 and VCAP cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP cells
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Concentration:0-10 μM
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Incubation Time:7 days
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Result:Inhibited the proliferation of LNCaPs with a GI50 value of 74 nM.
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Cell Line:LNCaP cells
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Concentration:0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM
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Incubation Time:24 h
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Result:Was able to inhibit the expression of AR target genes.
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Cell Line:C42 cells and VCAP cells
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Concentration:0.1 nM, 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM
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Incubation Time:24 h
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Result:Was able to degrade AR.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immunocompromised NOD SCID male mice implanted with C4-2 cell subcutaneous tumors[1].
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Dosage:30 mg/kg
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Administration:Oral gavage (p.o.); once daily; for 10 days
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Result:Degraded AR and inhibited tumor growth.
化学情報
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CAS 番号 2960179-55-7
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性状 Solid
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分子量 801.87
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分子式 C43H47F4N7O4
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Color White to off-white
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SMILES
COC1=CC(N2CCN(CC3CCN(C4=CC=C(C5CCN(C6=CC=C(C#N)C(C(F)(F)F)=C6F)CC5)C=C4)CC3)CC2)=CC7=C1C(N(C8CCC(NC8=O)=O)C7)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 50 mg/mL (62.35 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. 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. 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 (270 KB)
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SDS (251 KB)
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- Deutsch - DE (251 KB)
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- Portuguese - PT (251 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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2471 mL | 6.2354 mL | 12.4708 mL | 31.1771 mL |
| 5 mM | 0.2494 mL | 1.2471 mL | 2.4942 mL | 6.2354 mL | |
| 10 mM | 0.1247 mL | 0.6235 mL | 1.2471 mL | 3.1177 mL | |
| 15 mM | 0.0831 mL | 0.4157 mL | 0.8314 mL | 2.0785 mL | |
| 20 mM | 0.0624 mL | 0.3118 mL | 0.6235 mL | 1.5589 mL | |
| 25 mM | 0.0499 mL | 0.2494 mL | 0.4988 mL | 1.2471 mL | |
| 30 mM | 0.0416 mL | 0.2078 mL | 0.4157 mL | 1.0392 mL | |
| 40 mM | 0.0312 mL | 0.1559 mL | 0.3118 mL | 0.7794 mL | |
| 50 mM | 0.0249 mL | 0.1247 mL | 0.2494 mL | 0.6235 mL | |
| 60 mM | 0.0208 mL | 0.1039 mL | 0.2078 mL | 0.5196 mL |
AZ'3137 関連分類
HY-162702 関連分類
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