MS9449
Based on 1 Customer Validation
MS9449 is a potent PROTAC EGFR degrader, with Kd values of 17 nM and 10 nM for wild-type EGFR and mutant EGFRL858R, respectively, and a DC50 of 7.1 nM for EGFRDel19. MS9449 effectively induces the degradation of mutant EGFR through the ubiquitin-proteasome system (UPS) and the autophagy-lysosome pathway. MS9449 exhibits anticancer activity against non-small cell lung cancer. MS9449 can be applied in related research on non-small cell lung cancer.
(Pink: EGFR ligand (HY-W109039); Blue: VHL ligand (HY-139660); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.95%
- No. CAS: 2772612-96-9
- Fòrmula: C60H76ClFN10O8S
- Peso molecular:1151.82
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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
Descripciòn
IC50 & Target
[1]|
EGFR (WT) 17 nM (Kd) |
EGFR L858R 10 nM (Kd) |
VHL |
EGFRdel19 7.1 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC827 | DC50 |
7.1 nM
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EGFRDel19 degradation activity in human HCC-827 cells assessed by measuring EGFR protein levels.
EGFRDel19 degradation activity in human HCC-827 cells assessed by measuring EGFR protein levels.
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35675209 |
| HCC827 | GI50 |
0.25 μM
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Antiproliferative activity against human HCC-827 cells assessed as cell growth inhibition.
Antiproliferative activity against human HCC-827 cells assessed as cell growth inhibition.
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35675209 |
In Vitro
MS9449 binds to purified WT EGFR and EGFRL858R mutant EGFR with high affinity, displaying Kd values of 17 nM and 10 nM, respectively[1].
MS9449 potently and concentration-dependently degrades EGFRDel19 and inhibits its phosphorylation in HCC-827 cells, with a DC50 of 7.1 nM[1].
MS9449 (4-48 h) induces time-dependent degradation of EGFRDel19 in HCC-827 cells, with significant degradation detected within 4 h and sustained for up to 48 h[1].
MS9449 potently inhibits the proliferation of HCC-827 cells with a GI50 of 0.25 μM[1].
MS9449 (10-1000 nM; 16 h) potently inhibits proliferation of HCC827 NSCLC cells with a GI50 of 0.25 μM and binds to purified EGFRWT and EGFRL858R with Kd values of 17 nM and 10 nM, respectively[2].
MS9449-induced degradation of EGFRDel19 in HCC-827 cells depends on active cullin ring family E3 ubiquitin ligase complexes, the ubiquitin/proteasome system, binding to EGFR, and the autophagy/lysosome pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCC-827 cells
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Concentration:10, 100, 1000 nM
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Incubation Time:16 h
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Result:Effectively reduced the EGFR protein level.
Chemical Information
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No. CAS 2772612-96-9
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Appearance Solid
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Peso molecular 1151.82
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Fòrmula C60H76ClFN10O8S
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Color White to light yellow
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SMILES
O=C([C@H]1N(C([C@@H](C2=CC(C)=NO2)C(C)C)=O)C[C@H](O)C1)N[C@H](C3=CC=C(C4=C(C)N=CS4)C=C3)CC(NCCCCCCCCCCC(N5CCN(CCCOC6=CC7=C(NC8=CC=C(F)C(Cl)=C8)N=CN=C7C=C6OC)CC5)=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 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 200 mg/mL (173.64 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 (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 0.8682 mL | 4.3410 mL | 8.6819 mL | 21.7048 mL |
| 5 mM | 0.1736 mL | 0.8682 mL | 1.7364 mL | 4.3410 mL | |
| 10 mM | 0.0868 mL | 0.4341 mL | 0.8682 mL | 2.1705 mL | |
| 15 mM | 0.0579 mL | 0.2894 mL | 0.5788 mL | 1.4470 mL | |
| 20 mM | 0.0434 mL | 0.2170 mL | 0.4341 mL | 1.0852 mL | |
| 25 mM | 0.0347 mL | 0.1736 mL | 0.3473 mL | 0.8682 mL | |
| 30 mM | 0.0289 mL | 0.1447 mL | 0.2894 mL | 0.7235 mL | |
| 40 mM | 0.0217 mL | 0.1085 mL | 0.2170 mL | 0.5426 mL | |
| 50 mM | 0.0174 mL | 0.0868 mL | 0.1736 mL | 0.4341 mL | |
| 60 mM | 0.0145 mL | 0.0723 mL | 0.1447 mL | 0.3617 mL | |
| 80 mM | 0.0109 mL | 0.0543 mL | 0.1085 mL | 0.2713 mL | |
| 100 mM | 0.0087 mL | 0.0434 mL | 0.0868 mL | 0.2170 mL |
MS9449 Related Classifications
HY-147942 Related Classifications
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