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)).
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 2960179-55-7
- Formula: C43H47F4N7O4
- Molecular Weight:801.87
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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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
All PROTACs Isoforms
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Biological Activity
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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.
Chemical Information
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CAS No. 2960179-55-7
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Appearance Solid
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Molecular Weight 801.87
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 Related Classifications
HY-162702 Related Classifications
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