AMPTX-1
Based on 1 Customer Validation
AMPTX-1 is a selective, orally active, covalent reversible BRD9 molecular glue degrader with a DC50 of 0.05 nM. AMPTX-1 selectively recruits BRD9 to the E3 ligase DCAF16. AMPTX-1 forms a ternary complex with BRD9 and a reversible covalent adduct with Cys58 on the surface of DCAF16. AMPTX-1 mediates BRD9 degradation via the proteasome and Cullin RING E3 ligase pathways. AMPTX-1 can be used in the research of solid tumors and hematological malignancies.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.00%
- No. CAS: 3033019-04-1
- Fòrmula: C42H53N5O4
- Peso molecular:691.90
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
In Vitro
AMPTX-1 (6 h) potently degrades endogenous BRD9 in MV4-11 cells (DC50 = 0.5 nM, Dmax = 93%) and MCF-7 cells (DC50 = 2 nM, Dmax = 70%) following 6 h treatment, with a hook effect at concentrations above 100 nM[1].
AMPTX-1 (6 h) -induced BRD9 degradation in BRD9-HiBiT HEK293 cells is dependent on proteasome function, Cullin RING E3 ligase activity, and BRD9 engagement, as pre-treatment with MLN4924, Bortezomib, or BI-7273 blocks degradation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 3033019-04-1
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Appearance Solid
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Peso molecular 691.90
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Fòrmula C42H53N5O4
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Color White to off-white
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SMILES
N#C/C(C(N1CCC2=C(C1C)C=CC=C2CN3CCN(CC34CC4)CC5=C(OC)C=C(C6=CN(C)C(C(C)=C6C)=O)C=C5OC)=O)=C\C(C)(C)C
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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 (144.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (271 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 | 1.4453 mL | 7.2265 mL | 14.4530 mL | 36.1324 mL |
| 5 mM | 0.2891 mL | 1.4453 mL | 2.8906 mL | 7.2265 mL | |
| 10 mM | 0.1445 mL | 0.7226 mL | 1.4453 mL | 3.6132 mL | |
| 15 mM | 0.0964 mL | 0.4818 mL | 0.9635 mL | 2.4088 mL | |
| 20 mM | 0.0723 mL | 0.3613 mL | 0.7226 mL | 1.8066 mL | |
| 25 mM | 0.0578 mL | 0.2891 mL | 0.5781 mL | 1.4453 mL | |
| 30 mM | 0.0482 mL | 0.2409 mL | 0.4818 mL | 1.2044 mL | |
| 40 mM | 0.0361 mL | 0.1807 mL | 0.3613 mL | 0.9033 mL | |
| 50 mM | 0.0289 mL | 0.1445 mL | 0.2891 mL | 0.7226 mL | |
| 60 mM | 0.0241 mL | 0.1204 mL | 0.2409 mL | 0.6022 mL | |
| 80 mM | 0.0181 mL | 0.0903 mL | 0.1807 mL | 0.4517 mL | |
| 100 mM | 0.0145 mL | 0.0723 mL | 0.1445 mL | 0.3613 mL |
AMPTX-1 Related Classifications
HY-172615 Related Classifications
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