MT1
Based on 1 Customer Validation
MT1 is a bivalent chemical probe of BET bromodomains, with an IC50 of 0.789 nM for BRD4(1).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.69%
- No. CAS: 2060573-82-0
- Fòrmula: C54H66Cl2N10O9S2
- Peso molecular:1134.20
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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
Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
0.17 nM
Compound: 2
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Antiproliferative activity against human MV4-11 cells
Antiproliferative activity against human MV4-11 cells
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[PMID: 35714446] |
In Vitro
MT1 (100 nM, 24 h) significantly induces apoptosis via caspase-3 and PARP in MV4;11 cells[1].
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[1].
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Concentration:100 nM.
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Incubation Time:24 h.
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Result:Significant apoptosis was observed by caspase-3 and PARP cleavage after treatment.
In Vivo
MT1 exhibits terminal t1/2 of 2.70 h in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Leukemia xenograft models[1].
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Dosage:44.2 and 22.1 µmol/kg.
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Administration:Intraperitoneally for 14 subsequent days.
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Result:Significantly reduced leukemic burden over the course of the study compared to either vehicle or JQ1.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2060573-82-0
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Appearance Solid
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Peso molecular 1134.20
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Fòrmula C54H66Cl2N10O9S2
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Color Off-white to light yellow
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SMILES
CC1=NN=C2N1C3=C(C(C4=CC=C(C=C4)Cl)=N[C@H]2CC(NCCOCCOCCOCCOCCOCCOCCOCCNC(C[C@@H]5N=C(C6=C(N7C5=NN=C7C)SC(C)=C6C)C8=CC=C(C=C8)Cl)=O)=O)C(C)=C(C)S3
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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 : 150 mg/mL (132.25 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: ≥ 7.5 mg/mL (6.61 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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: 7.5 mg/mL (6.61 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 7.5 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 (75.0 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 (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 0.8817 mL | 4.4084 mL | 8.8168 mL | 22.0420 mL |
| 5 mM | 0.1763 mL | 0.8817 mL | 1.7634 mL | 4.4084 mL | |
| 10 mM | 0.0882 mL | 0.4408 mL | 0.8817 mL | 2.2042 mL | |
| 15 mM | 0.0588 mL | 0.2939 mL | 0.5878 mL | 1.4695 mL | |
| 20 mM | 0.0441 mL | 0.2204 mL | 0.4408 mL | 1.1021 mL | |
| 25 mM | 0.0353 mL | 0.1763 mL | 0.3527 mL | 0.8817 mL | |
| 30 mM | 0.0294 mL | 0.1469 mL | 0.2939 mL | 0.7347 mL | |
| 40 mM | 0.0220 mL | 0.1102 mL | 0.2204 mL | 0.5510 mL | |
| 50 mM | 0.0176 mL | 0.0882 mL | 0.1763 mL | 0.4408 mL | |
| 60 mM | 0.0147 mL | 0.0735 mL | 0.1469 mL | 0.3674 mL | |
| 80 mM | 0.0110 mL | 0.0551 mL | 0.1102 mL | 0.2755 mL | |
| 100 mM | 0.0088 mL | 0.0441 mL | 0.0882 mL | 0.2204 mL |
MT1 Related Classifications
HY-111976 Related Classifications
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