LO-4-25
Based on 1 Customer Validation
LO-4-25 is a CUL4DCAF16 based covalent PROTAC-like degrader. LO-4-25 induces degradation of the androgen receptor (AR) and androgen receptor truncation variant AR-V7. LO-4-25 covalently targets cysteine residues on CUL4DCAF16 to mediate degradation of neo-substrates. LO-4-25 triggers proteasome-dependent degradation of target proteins via CUL4DCAF16-mediated ubiquitination. LO-4-25 can be used for the research of androgen-independent prostate cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.68%
- Formel: C32H37ClN6O5S
- Molecular Weight:653.19
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Speicherung:Powder -20°C, 3 years , 4°C, 2 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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
In Vitro
LO-4-25 (1-10 μM; 24 h) potently degrades both AR and AR-V7 in 22Rv1 cells in a CUL4DCAF16-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:22Rv1 androgen-independent prostate cancer cells
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Concentration:1 μM, 10 μM
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Incubation Time:24 h
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Result:Induced robust degradation of both AR and AR-V7 in 22Rv1 cells.
Completely attenuated degradation of AR and AR-V7 in 22Rv1 cells with DCAF16 knockdown via siRNA transfection.
Chemical Information
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Appearance Solid
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Molecular Weight 653.19
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Formel C32H37ClN6O5S
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Color Off-white to light yellow
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SMILES
O=C(NC1=CC(Cl)=CN=C1)/C=C/C(N2CCN(CC2)C(CCCCCOC3=CC=C(C=C3)C4=CSC(N5CCOCC5)=N4)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (153.09 mM; ultrasonic and warming and heat to 60°C; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Reinheit & Dokumentation
Verweise
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 | 1.5309 mL | 7.6547 mL | 15.3095 mL | 38.2737 mL |
| 5 mM | 0.3062 mL | 1.5309 mL | 3.0619 mL | 7.6547 mL | |
| 10 mM | 0.1531 mL | 0.7655 mL | 1.5309 mL | 3.8274 mL | |
| 15 mM | 0.1021 mL | 0.5103 mL | 1.0206 mL | 2.5516 mL | |
| 20 mM | 0.0765 mL | 0.3827 mL | 0.7655 mL | 1.9137 mL | |
| 25 mM | 0.0612 mL | 0.3062 mL | 0.6124 mL | 1.5309 mL | |
| 30 mM | 0.0510 mL | 0.2552 mL | 0.5103 mL | 1.2758 mL | |
| 40 mM | 0.0383 mL | 0.1914 mL | 0.3827 mL | 0.9568 mL | |
| 50 mM | 0.0306 mL | 0.1531 mL | 0.3062 mL | 0.7655 mL | |
| 60 mM | 0.0255 mL | 0.1276 mL | 0.2552 mL | 0.6379 mL | |
| 80 mM | 0.0191 mL | 0.0957 mL | 0.1914 mL | 0.4784 mL | |
| 100 mM | 0.0153 mL | 0.0765 mL | 0.1531 mL | 0.3827 mL |
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