ARCC-4
Based on 3 publication(s) in Google Scholar
ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.88%
- No. CAS: 1973403-00-7
- Fòrmula: C53H56F3N7O7S2
- Peso molecular:1024.18
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-70002
EnzalutamideAndrogen Receptor Antagonist -
HY-138641
BavdegalutamideAR PROTAC Degrader -
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ARD-2128PROTAC AR Degrader -
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LuxdegalutamidePROTAC -
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BicalutamideAndrogen Receptor Inhibitor -
HY-139436
ARD-2585Androgen Receptor PROTAC Degrader -
HY-16060
ApalutamideAR Antagonist -
HY-135794
11-KetodihydrotestosteroneAndrogen Receptor Agonist -
HY-15194
DimethylcurcuminAndrogen Receptor Inhibitor -
HY-133020
ARD-266PROTAC Androgen Receptor Degrader -
HY-111024
2,2,5,7,8-Pentamethyl-6-ChromanolAndrogen Receptor Modulator -
HY-137448
RezvilutamideAndrogen Receptor Antagonist
Publications Citing Use of MedChemExpress (MCE) ARCC-4
MoreVer todos los productos específicos de isoformas PROTACs
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
VHL |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | DC50 |
<=50 μM
Compound: Example 75
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Protac activity at E3 ubiquitin-protein ligase/AR in human LNCAP cells assessed as induction of AR degradation after 24 hrs by ELISA
Protac activity at E3 ubiquitin-protein ligase/AR in human LNCAP cells assessed as induction of AR degradation after 24 hrs by ELISA
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[PMID: 32550986] |
| VCaP | DC50 |
<=50 μM
Compound: Example 75
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Protac activity at E3 ubiquitin-protein ligase/AR in human VCAP cells assessed as induction of AR degradation after 24 hrs by ELISA
Protac activity at E3 ubiquitin-protein ligase/AR in human VCAP cells assessed as induction of AR degradation after 24 hrs by ELISA
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[PMID: 32550986] |
| VCaP | DC50 |
5 nM
Compound: 60; ARCC-4
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Protac activity against VHL/androgen receptor in human VCaP cells assessed as induction of androgen receptor protein degradation by Western blot analysis
Protac activity against VHL/androgen receptor in human VCaP cells assessed as induction of androgen receptor protein degradation by Western blot analysis
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[PMID: 31035238] |
In Vitro
ARCC-4 induces apoptosis and inhibiting proliferation of AR-amplified prostate cancer cells[1].
ARCC-4 enhances protein-protein interactions between AR and VHL, thereby promoting the association of the trimeric complex[1].
ARCC-4 (0.1-10,000 nM; 20 hours) potently degrades AR with a D50 of 5 nM and Dmax of over 95%[1].
ARCC-4 (100 nM; 12 hours) shows near complete AR degradation (>98%) in prostate cancer cells[1].
ARCC-4 selectively degrades AR via the proteasome but not PR-A or PR-B suppression[1].
ARCC-4 shows efficacy against clinically relevant AR mutations[1].
ARCC-4 maintains activity despite elevated androgen levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:VCaP cells
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Concentration:0.1 nM, 1 nM, 10 nM, 50 nM, 100 nM, 0.5μM, 1μM, 10 μM
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Incubation Time:20 hours
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Result:Potently degrades AR
Chemical Information
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No. CAS 1973403-00-7
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Appearance Solid
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Peso molecular 1024.18
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Fòrmula C53H56F3N7O7S2
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Color White to off-white
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SMILES
O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H]3N(C([C@H](C(C)(C)C)NC(COCCCCOC4=CC=C(C5=CC=C(N(C(N6C7=CC=C(C#N)C(C(F)(F)F)=C7)=S)C(C)(C)C6=O)C=C5)C=C4)=O)=O)C[C@H](O)C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Am J Pathol
Testosterone-Induced H3K27 Deacetylation Participates in Granulosa Cell Proliferation Suppression and Pathogenesis of Polycystic Ovary Syndrome. [Abstract]2024 Dec;194(12):2326-2340. PMID: 39243944 -
Solvente y solubilidad
In Vitro:
DMSO : 200 mg/mL (195.28 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (4.88 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (4.88 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9764 mL | 4.8820 mL | 9.7639 mL | 24.4098 mL |
| 5 mM | 0.1953 mL | 0.9764 mL | 1.9528 mL | 4.8820 mL | |
| 10 mM | 0.0976 mL | 0.4882 mL | 0.9764 mL | 2.4410 mL | |
| 15 mM | 0.0651 mL | 0.3255 mL | 0.6509 mL | 1.6273 mL | |
| 20 mM | 0.0488 mL | 0.2441 mL | 0.4882 mL | 1.2205 mL | |
| 25 mM | 0.0391 mL | 0.1953 mL | 0.3906 mL | 0.9764 mL | |
| 30 mM | 0.0325 mL | 0.1627 mL | 0.3255 mL | 0.8137 mL | |
| 40 mM | 0.0244 mL | 0.1220 mL | 0.2441 mL | 0.6102 mL | |
| 50 mM | 0.0195 mL | 0.0976 mL | 0.1953 mL | 0.4882 mL | |
| 60 mM | 0.0163 mL | 0.0814 mL | 0.1627 mL | 0.4068 mL | |
| 80 mM | 0.0122 mL | 0.0610 mL | 0.1220 mL | 0.3051 mL | |
| 100 mM | 0.0098 mL | 0.0488 mL | 0.0976 mL | 0.2441 mL |
ARCC-4 Related Classifications
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