PROTAC EGFR degrader 15
Based on 1 Customer Validation
PROTAC EGFR degrader 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC).
(Pink: EGFR ligand (HY-W109039); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.23%
- Formula: C45H52ClFN8O7
- Molecular Weight:871.40
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cereblon |
PROTAC EGFR degrader 15 (Compound P-G) (0-1 μM, 24 h + washout 0-72 h) effectively and sustainably induces EGFR protein degradation via both ubiquitin/proteasome pathway and autophagy/lysosome degradation pathway both in HCC-827 parental and EGFR-tyrosine kinase inhibitors (EGFR-TKIs) resistant cells[1].
PROTAC EGFR degrader 15 (0.5 μM, 44-64°C, 2 h) promotes energy production in HCC-827-ER (Erlotinib (HY-50896) resistance) resistance cells by targeting ETFA[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, HCC-827-GR, HCC-827-ER, HCC-827-OR and HCC-827-RR cells
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Concentration:0, 0.1, 0.5 and 1 μM
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Incubation Time:24 h + washout 0, 6, 12, 24, 48 and 72 h
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Result:Exhibited concentration-dependent and long lasting degradation of EGFR and p-EGFR in all cell lines.
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Cell Line:HCC-827 cells
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Concentration:0.5 μM
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Incubation Time:2 h
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Result:Resulted in a significant increase in the thermal stability of ETFA at various temperatures both in intact cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCC-827-GR xenografts model established in male BALB/c nude mice (20 g)[1]
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Dosage:30 mg/kg
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Administration:Intraperitoneal injection (i.p.), every other day for 2 weeks
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Result:Suppressed the HCC-827-GR xenografts tumor and the tumor growth inhibition (TGI) was 48.24 %.
Was no statistical differences in organ indices between vehicle treated group.
Chemical Information
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Appearance Solid
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Molecular Weight 871.40
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Formula C45H52ClFN8O7
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Color White to off-white
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SMILES
O=C(N1)CCC(N2C(C(C(NC(CCCCCCCCCN3CCN(CCCOC4=CC(C(NC5=CC(Cl)=C(F)C=C5)=NC=N6)=C6C=C4OC)CC3)=O)=CC=C7)=C7C2=O)=O)C1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (114.76 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)
Purity & Documentation
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Data Sheet (274 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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Handling Instructions (2659 KB)
References
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 | 1.1476 mL | 5.7379 mL | 11.4758 mL | 28.6895 mL |
| 5 mM | 0.2295 mL | 1.1476 mL | 2.2952 mL | 5.7379 mL | |
| 10 mM | 0.1148 mL | 0.5738 mL | 1.1476 mL | 2.8689 mL | |
| 15 mM | 0.0765 mL | 0.3825 mL | 0.7651 mL | 1.9126 mL | |
| 20 mM | 0.0574 mL | 0.2869 mL | 0.5738 mL | 1.4345 mL | |
| 25 mM | 0.0459 mL | 0.2295 mL | 0.4590 mL | 1.1476 mL | |
| 30 mM | 0.0383 mL | 0.1913 mL | 0.3825 mL | 0.9563 mL | |
| 40 mM | 0.0287 mL | 0.1434 mL | 0.2869 mL | 0.7172 mL | |
| 50 mM | 0.0230 mL | 0.1148 mL | 0.2295 mL | 0.5738 mL | |
| 60 mM | 0.0191 mL | 0.0956 mL | 0.1913 mL | 0.4782 mL | |
| 80 mM | 0.0143 mL | 0.0717 mL | 0.1434 mL | 0.3586 mL | |
| 100 mM | 0.0115 mL | 0.0574 mL | 0.1148 mL | 0.2869 mL |
PROTAC EGFR degrader 15 Related Classifications
HY-175839 Related Classifications
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