MLT-231
Based on 1 Customer Validation
MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.55%
- No. CAS: 2682102-10-7
- Fòrmula: C19H19ClF3N7O2
- Peso molecular:469.85
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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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BJAB | IC50 |
2 μM
Compound: 27; MLT-231
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Antiproliferation activity against human BJAB cells assessed as reduction in cell viability incubated for 14 days by resazurin dye-based fluorescence analysis
Antiproliferation activity against human BJAB cells assessed as reduction in cell viability incubated for 14 days by resazurin dye-based fluorescence analysis
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[PMID: 33252239] |
| BMDM | IC50 |
>10 μM
Compound: 27; MLT-231
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Cytotoxicity against mouse Bone marrow-derived macrophage cells assessed as reduction in cell viability by [3H]-thymidine incorporation assay
Cytotoxicity against mouse Bone marrow-derived macrophage cells assessed as reduction in cell viability by [3H]-thymidine incorporation assay
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[PMID: 33252239] |
| OCI-Ly3 | IC50 |
>10 μM
Compound: 27; MLT-231
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Antiproliferation activity against human OCI-LY3 cells assessed as reduction in cell viability incubated for 14 days by resazurin dye-based fluorescence analysis
Antiproliferation activity against human OCI-LY3 cells assessed as reduction in cell viability incubated for 14 days by resazurin dye-based fluorescence analysis
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[PMID: 33252239] |
| PBMC | IC50 |
0.19 μM
Compound: 27; MLT-231
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Inhibition of mixed lymphocyte reaction in human PBMC cells assessed as reduction in [3H]-thymidine incorporation measured after 5 days in presence of Il-7 by microbeta counting method
Inhibition of mixed lymphocyte reaction in human PBMC cells assessed as reduction in [3H]-thymidine incorporation measured after 5 days in presence of Il-7 by microbeta counting method
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[PMID: 33252239] |
In Vitro
MLT-231 (19.5-10000 nM) inhibits the proliferation of OCI-Ly3 cells. MLT-231 (50-5000 nM; 24 hours) leads to accumulation of the uncleaved form of its substrates CYLD, BCL10, and RELB while expression of the NF-κB target gene IRF4 is suppressed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OCI-Ly3 cells
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Concentration:50-5000 nM
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Incubation Time:24 hours
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Result:NF-κB target gene IRF4 was suppressed.
In Vivo
MLT-231 (1 mg/kg; i.v.; BALB/c mice) treatment shows the CL, t1/2, and Vss are 11 mL/min/kg, 1.9 hours, and 1.5 L/kg, respectively[1].
MLT-231 (1 mg/kg; i.v.; Sprague-Dawley rats) treatment shows the CL, t1/2, and Vss are 41 mL/min/kg, 3.2 hours, and 9.4 L/kg, respectively[1].
MLT-231 (3 mg/kg; p.o.; BALB/c mice) treatment shows the AUC0-24, Cmax and F are 3096 nM/h, 549 nM, and 99%, respectively[1].
MLT-231 (3 mg/kg; p.o.; Sprague-Dawley rats) treatment shows the AUC0-24, Cmax and F are 547 nM/h, 46 nM, and 61%, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Scid-beige mice (OCI-Ly10 ABC-DLBCL type xenograft model)[1]
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Dosage:10, 30, and 100 mg/kg
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Administration:P.o.; bid schedule for 2 weeks
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Result:Led to tumor stasis, while being well tolerated.
Chemical Information
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No. CAS 2682102-10-7
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Appearance Solid
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Peso molecular 469.85
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Fòrmula C19H19ClF3N7O2
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Color White to off-white
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SMILES
O=C(NC1=C(N2[C@@H](C)COC[C@@H]2C)N3C(N=C1)=CC(Cl)=N3)NC4=CC=NC(C(F)(F)F)=C4
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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 : 110 mg/mL (234.12 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: ≥ 6 mg/mL (12.77 mM); Clear solution
This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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.
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 (273 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 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 | 2.1283 mL | 10.6417 mL | 21.2834 mL | 53.2085 mL |
| 5 mM | 0.4257 mL | 2.1283 mL | 4.2567 mL | 10.6417 mL | |
| 10 mM | 0.2128 mL | 1.0642 mL | 2.1283 mL | 5.3208 mL | |
| 15 mM | 0.1419 mL | 0.7094 mL | 1.4189 mL | 3.5472 mL | |
| 20 mM | 0.1064 mL | 0.5321 mL | 1.0642 mL | 2.6604 mL | |
| 25 mM | 0.0851 mL | 0.4257 mL | 0.8513 mL | 2.1283 mL | |
| 30 mM | 0.0709 mL | 0.3547 mL | 0.7094 mL | 1.7736 mL | |
| 40 mM | 0.0532 mL | 0.2660 mL | 0.5321 mL | 1.3302 mL | |
| 50 mM | 0.0426 mL | 0.2128 mL | 0.4257 mL | 1.0642 mL | |
| 60 mM | 0.0355 mL | 0.1774 mL | 0.3547 mL | 0.8868 mL | |
| 80 mM | 0.0266 mL | 0.1330 mL | 0.2660 mL | 0.6651 mL | |
| 100 mM | 0.0213 mL | 0.1064 mL | 0.2128 mL | 0.5321 mL |
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