SR-1114
Based on 1 Customer Validation
SR-1114 is a ENL PROTAC degrader, with DC50 values of 150 nM, 311 nM and 1.65 μM in MV4;11, MOLM-13 and OCI/AML-2 cells, respectively. SR-1114 has an IC50 of 155 nM against the human CRL4CRBN complex. SR-1114 can be used in research related to acute leukemia and acute myeloid leukemia.
(Pink: ENL YEATS domain ligand (HY-145409); Blue: Cereblon ligand (HY-14658); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.22%
- No. CAS: 2769141-82-2
- Fòrmula: C39H42N8O11S
- Peso molecular:830.86
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Cereblon |
In Vitro
SR-1114 (10 μM; 4-16 h) drives potent, selective degradation of ENL, suppresses ENL target proteins, induces CD11b expression, and causes weak off-target degradation of IKZF1 in MV4;11 cells[1].
SR-1114 binds CRBN-DDB1 independently with an IC50 of 155 nM, and shows weak cooperative binding (α = 2.3) in the presence of ENL YEATS domain, with an IC50 of 68 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4;11 cells
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Concentration:9, 30, 80, 250, 740 nm and 2, 7, 20 μM
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Incubation Time:4 h
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Result:Inhibited the levels of ENL.
Chemical Information
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No. CAS 2769141-82-2
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Appearance Solid
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Peso molecular 830.86
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Fòrmula C39H42N8O11S
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Color White to off-white
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SMILES
O=C(NCCOCCOCCNS(=O)(NC1=CC=CC(C2=CN3C=C(C=CC3=N2)C(NC4CCC4)=O)=C1)=O)COC5=CC=CC6=C5C(N(C6=O)C7CCC(NC7=O)=O)=O
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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 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (120.36 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)
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: 2.5 mg/mL (3.01 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (3.01 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Garnar-Wortzel L, et al. Chemical Inhibition of ENL/AF9 YEATS Domains in Acute Leukemia. ACS central science. 2021 May 26;7(5):815-830. [Content Brief]
[2].
Shaum JB, et al. High-throughput ligand diversification to discover chemical inducers of proximity. Nat Chem Biol. 2026 Feb 16:10.1038/s41589-025-02137-2.
[Content Brief]
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 | 1.2036 mL | 6.0179 mL | 12.0357 mL | 30.0893 mL |
| 5 mM | 0.2407 mL | 1.2036 mL | 2.4071 mL | 6.0179 mL | |
| 10 mM | 0.1204 mL | 0.6018 mL | 1.2036 mL | 3.0089 mL | |
| 15 mM | 0.0802 mL | 0.4012 mL | 0.8024 mL | 2.0060 mL | |
| 20 mM | 0.0602 mL | 0.3009 mL | 0.6018 mL | 1.5045 mL | |
| 25 mM | 0.0481 mL | 0.2407 mL | 0.4814 mL | 1.2036 mL | |
| 30 mM | 0.0401 mL | 0.2006 mL | 0.4012 mL | 1.0030 mL | |
| 40 mM | 0.0301 mL | 0.1504 mL | 0.3009 mL | 0.7522 mL | |
| 50 mM | 0.0241 mL | 0.1204 mL | 0.2407 mL | 0.6018 mL | |
| 60 mM | 0.0201 mL | 0.1003 mL | 0.2006 mL | 0.5015 mL | |
| 80 mM | 0.0150 mL | 0.0752 mL | 0.1504 mL | 0.3761 mL | |
| 100 mM | 0.0120 mL | 0.0602 mL | 0.1204 mL | 0.3009 mL |
SR-1114 Related Classifications
HY-115881 Related Classifications
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