AF151
Based on 1 Customer Validation
AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML). (Pink: METTL3 Ligand (HY-174874); Blue: VHL Ligand (HY-125845); Black: Linker; VHL Ligand+Linker (HY-174875)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.87%
- Fòrmula: C61H70N8O6S
- Peso molecular:1043.32
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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
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Bcl-2 |
VHL |
Mcl-1 |
AF151 (0-10 μM, 0-72 h) can efficiently degrade METTL3 protein in a time-dependent manner and significantly inhibit cell growth of MOLM-13 cells (DC50 = 0.43 μM, IC50 = 0.45 μM)[1].
AF151 (2 μM, 24-48 h) can significantly reduce m6A levels in MOLM-13 cells[1].
AF151 (0.1-5 μM, 48 h) can dose dependently induce cell apoptosis and reduce the level of anti apoptotic proteins in MOLM-13 cells[1].
AF151 (72 h) can work synergistically with Venetoclax (HY-15531) in MOLM-13 cells[1].
AF151 (0.001-10 μM) can promote the binding of METTL3 and VHL (AF151 = 363 nM, AF151-METTL3 = 79.9 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-13 cells
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Concentration:0.1-10 μM
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Incubation Time:72 h
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Result:Significantly inhibited cell growth with the IC50 of 0.45 μM, superior to STM2457 (HY-134836) (IC50 = 1.82 μM) and WD6305 (HY-160415) (IC50 = 0.78 μM).
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Cell Line:MOLM-13 cells
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Concentration:2 μM
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Incubation Time:48 h
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Result:Decreased the protein level of Mcl-1 and Bcl-2.
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Cell Line:MOLM-13 cells
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Concentration:2 μM
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Incubation Time:24-48 h
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Result:Did not cause significant changes in the expression of METTL3 and METTL14 genes.
Chemical Information
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Appearance Solid
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Peso molecular 1043.32
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Fòrmula C61H70N8O6S
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Color Light yellow to yellow
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SMILES
CC1=C(C2=CC=C(CNC([C@H]3N(C([C@@H](NC(CCC4=CC=C(C5=CC=C(COC6=CN=CC(C(NCC7=CC(NC(CN8CCC(C)(C)CC8)=C9)=C9C=C7)=O)=C6)C=C5)C=C4)=O)C(C)(C)C)=O)C[C@H](O)C3)=O)C=C2)SC=N1
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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
DMSO : 100 mg/mL (95.85 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)
Pureza y Documentación
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Ficha de datos (272 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 |
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| DMSO | 1 mM | 0.9585 mL | 4.7924 mL | 9.5848 mL | 23.9620 mL |
| 5 mM | 0.1917 mL | 0.9585 mL | 1.9170 mL | 4.7924 mL | |
| 10 mM | 0.0958 mL | 0.4792 mL | 0.9585 mL | 2.3962 mL | |
| 15 mM | 0.0639 mL | 0.3195 mL | 0.6390 mL | 1.5975 mL | |
| 20 mM | 0.0479 mL | 0.2396 mL | 0.4792 mL | 1.1981 mL | |
| 25 mM | 0.0383 mL | 0.1917 mL | 0.3834 mL | 0.9585 mL | |
| 30 mM | 0.0319 mL | 0.1597 mL | 0.3195 mL | 0.7987 mL | |
| 40 mM | 0.0240 mL | 0.1198 mL | 0.2396 mL | 0.5990 mL | |
| 50 mM | 0.0192 mL | 0.0958 mL | 0.1917 mL | 0.4792 mL | |
| 60 mM | 0.0160 mL | 0.0799 mL | 0.1597 mL | 0.3994 mL | |
| 80 mM | 0.0120 mL | 0.0599 mL | 0.1198 mL | 0.2995 mL |
AF151 Related Classifications
HY-174873 Related Classifications
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