PROTAC AR/AR-V7 degrader-1
Based on 1 Customer Validation
PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.72%
- CAS No.: 2841308-96-9
- Formula: C24H19F4N5O2
- Molecular Weight:485.43
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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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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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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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Apoptosis Compound Library
HY-L003
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GPCR/G Protein Compound Library
HY-L006
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Neuronal Signaling Compound Library
HY-L013
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Anti-Cancer Compound Library
HY-L025
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Covalent Screening Library
HY-L036
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Neurotransmitter Receptor Compound Library
HY-L062
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Antidepressant Compound Library
HY-L108
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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PROTAC Library
HY-L151
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Cell Death Library
HY-L162
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MCE Bioactive Compound Library
HY-L001V
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Covalent Screening Library Plus
HY-L036P
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
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Lactylation Compound Library
HY-L249
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
0.9 μM
Compound: 27c
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Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 38512060] |
| DU-145 | IC50 |
>50 μM
Compound: 27c
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Antiproliferative activity against AR-negative human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against AR-negative human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 38512060] |
| L02 | IC50 |
>100 μM
Compound: 27c
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Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 38512060] |
| LNCaP | IC50 |
1.4 μM
Compound: 27c
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Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 38512060] |
PROTAC AR/AR-V7 degrader-1 (27c) effectively suppresses transcriptional activity of the AR signaling pathway. PROTAC AR/AR-V7 degrader-1 (27c) exhibits an IC50 of 0.9 μM in 22RV1 cells[1].
PROTAC AR/AR-V7 degrader-1 (27c) overcomes drug resistance in advanced PCa expressing AR splice variants[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2841308-96-9
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Appearance Solid
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Molecular Weight 485.43
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Formula C24H19F4N5O2
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Color Off-white to yellow
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SMILES
O=C1C(C)(C)N(CCNC2=C(C=CC=N3)C3=C(F)C=C2)C(N1C4=CC(C(F)(F)F)=C(C#N)C=C4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (206.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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). 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). 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 (272 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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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 (protect from light). 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 | 2.0600 mL | 10.3001 mL | 20.6003 mL | 51.5007 mL |
| 5 mM | 0.4120 mL | 2.0600 mL | 4.1201 mL | 10.3001 mL | |
| 10 mM | 0.2060 mL | 1.0300 mL | 2.0600 mL | 5.1501 mL | |
| 15 mM | 0.1373 mL | 0.6867 mL | 1.3734 mL | 3.4334 mL | |
| 20 mM | 0.1030 mL | 0.5150 mL | 1.0300 mL | 2.5750 mL | |
| 25 mM | 0.0824 mL | 0.4120 mL | 0.8240 mL | 2.0600 mL | |
| 30 mM | 0.0687 mL | 0.3433 mL | 0.6867 mL | 1.7167 mL | |
| 40 mM | 0.0515 mL | 0.2575 mL | 0.5150 mL | 1.2875 mL | |
| 50 mM | 0.0412 mL | 0.2060 mL | 0.4120 mL | 1.0300 mL | |
| 60 mM | 0.0343 mL | 0.1717 mL | 0.3433 mL | 0.8583 mL | |
| 80 mM | 0.0258 mL | 0.1288 mL | 0.2575 mL | 0.6438 mL | |
| 100 mM | 0.0206 mL | 0.1030 mL | 0.2060 mL | 0.5150 mL |
PROTAC AR/AR-V7 degrader-1 Related Classifications
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