MS154
Based on 1 Customer Validation
MS154 is a first-in-class E3 ligase cereblon-recruited EGFR degrader with Kd values of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutant, respectively. MS154 potently induces degradation of mutant, but not wild-type, EGFR in cancer cell lines in an E3 ligase-dependent manner. MS154 exhibits anticancer effects against lung cancer (blue: E3 ligase ligand (HY-103596); black: linker (HY-W096167); pink: EGFR ligand (HY-168305)).
(Pink: EGFR ligand (HY-168305); Blue: Cereblon ligand (HY-103596); Black: linker (HY-W096167)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.71%
- No. CAS: 2550393-21-8
- Fòrmula: C46H54ClFN8O8
- Peso molecular:901.42
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Almacenamiento:Powder -20°C, 3 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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Cereblon |
EGFR (WT) 1.8 nM (Kd) |
EGFRL858R 3.8 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| HCC827 | DC50 |
11 nM
Compound: 10; MS154
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Protac activity at CRBN/EGFR exon 19 deletion mutant in human HCC827 cells assessed as induction of EGFR degradation treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis
Protac activity at CRBN/EGFR exon 19 deletion mutant in human HCC827 cells assessed as induction of EGFR degradation treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis
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[PMID: 31895569] |
MS154 exhibits a high binding affinity to EGFR WT (Kd = 1.8 nM) and a 5-fold weaker binding affinity to EGFR L858R mutant (Kd = 3.8 nM)[1].
MS154 (1 nM-10 μM; 16 h) potently induces concentration-dependent degradation of mutant EGFR (EGFR e19d in HCC-827 cells, EGFR L858R in H3255 cells) with DC50 values of 11 nM (HCC-827) and 25 nM (H3255)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2550393-21-8
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Appearance Solid
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Peso molecular 901.42
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Fòrmula C46H54ClFN8O8
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Color Off-white to light yellow
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SMILES
O=C1NC(C(CC1)N2C(C3=C(C2=O)C(OCCCCCCCCNC(CCN4CCN(CCCOC5=CC6=C(NC7=CC=C(C(Cl)=C7)F)N=CN=C6C=C5OC)CC4)=O)=CC=C3)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (110.94 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 (269 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 | 1.1094 mL | 5.5468 mL | 11.0936 mL | 27.7340 mL |
| 5 mM | 0.2219 mL | 1.1094 mL | 2.2187 mL | 5.5468 mL | |
| 10 mM | 0.1109 mL | 0.5547 mL | 1.1094 mL | 2.7734 mL | |
| 15 mM | 0.0740 mL | 0.3698 mL | 0.7396 mL | 1.8489 mL | |
| 20 mM | 0.0555 mL | 0.2773 mL | 0.5547 mL | 1.3867 mL | |
| 25 mM | 0.0444 mL | 0.2219 mL | 0.4437 mL | 1.1094 mL | |
| 30 mM | 0.0370 mL | 0.1849 mL | 0.3698 mL | 0.9245 mL | |
| 40 mM | 0.0277 mL | 0.1387 mL | 0.2773 mL | 0.6934 mL | |
| 50 mM | 0.0222 mL | 0.1109 mL | 0.2219 mL | 0.5547 mL | |
| 60 mM | 0.0185 mL | 0.0924 mL | 0.1849 mL | 0.4622 mL | |
| 80 mM | 0.0139 mL | 0.0693 mL | 0.1387 mL | 0.3467 mL | |
| 100 mM | 0.0111 mL | 0.0555 mL | 0.1109 mL | 0.2773 mL |
MS154 Related Classifications
HY-141640 Related Classifications
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