SR-0813
Based on 1 Customer Validation
SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 2597186-19-9
- Formula: C25H32N6O3S
- Molecular Weight:496.62
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Biological Activity
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ENL YEATS domain 25 nM (IC50) |
ENL YEATS domain 205 nM (EC50) |
AF9 YEATS domain 311 nM (IC50) |
AF9 YEATS domain 76 nM (EC50) |
ENL YEATS domain 30 nM (Kd) |
MAP3K19 3.5 μM (Kd) |
SR-0813 (compound 10; 0, 1, 10 μM; 4 h) dose-dependent evicts ENL from known ENL binding sites, including the HOXA10 gene body and MYB promoter in MV4;11 cells[1].
SR-0813 (0, 1, 10 μM; 0, 24, 48, 72 h) downregulates the transcript levels of HOXA9, MEIS1, and MYC, and increases the abundance of the ITGAM transcript in MV4;11 cells[1].
SR-0813 (0, 1, 10 μM; approximately 2 weeks) inhibits the growth of multiple lineage leukemia (MLL)-fusion leukemia cell lines (MV4;11, MOLM-13, OCI/AML-2) and HB11;19 cells[1].
SR-0813 (1 μM, 4h) does not elicit global changes in gene expression in MV4;11 cells, but produces a strikingly selective suppression of ENL target genes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MLL-fusion leukemia cell lines: MV4;11 (MLL-AF4 AML), MOLM-13 (MLL-AF9 AML), and OCI/AML-2 (MLL-AF6 AML), which are sensitive to the genetic loss of ENL.
HB11;19 cells, which harboring an MLL-ENL fusion. -
Concentration:0, 1, 10 μM
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Incubation Time:Approximately 2 weeks
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Result:Inhibited the growth of cells.
Chemical Information
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CAS No. 2597186-19-9
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Appearance Solid
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Molecular Weight 496.62
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Formula C25H32N6O3S
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Color White to off-white
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SMILES
O=C(C1=CN2C=C(C3=CC(NS(=O)(NCCN4CCCCC4)=O)=CC=C3)N=C2C=C1)NC5CCC5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (201.36 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)
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 (5.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
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.
Purity & Documentation
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Data Sheet (272 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)
- 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 | 2.0136 mL | 10.0681 mL | 20.1361 mL | 50.3403 mL |
| 5 mM | 0.4027 mL | 2.0136 mL | 4.0272 mL | 10.0681 mL | |
| 10 mM | 0.2014 mL | 1.0068 mL | 2.0136 mL | 5.0340 mL | |
| 15 mM | 0.1342 mL | 0.6712 mL | 1.3424 mL | 3.3560 mL | |
| 20 mM | 0.1007 mL | 0.5034 mL | 1.0068 mL | 2.5170 mL | |
| 25 mM | 0.0805 mL | 0.4027 mL | 0.8054 mL | 2.0136 mL | |
| 30 mM | 0.0671 mL | 0.3356 mL | 0.6712 mL | 1.6780 mL | |
| 40 mM | 0.0503 mL | 0.2517 mL | 0.5034 mL | 1.2585 mL | |
| 50 mM | 0.0403 mL | 0.2014 mL | 0.4027 mL | 1.0068 mL | |
| 60 mM | 0.0336 mL | 0.1678 mL | 0.3356 mL | 0.8390 mL | |
| 80 mM | 0.0252 mL | 0.1259 mL | 0.2517 mL | 0.6293 mL | |
| 100 mM | 0.0201 mL | 0.1007 mL | 0.2014 mL | 0.5034 mL |
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