EGFR-IN-8
Based on 1 Customer Validation
EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.01%
- No. CAS: 2407957-87-1
- Fòrmula: C32H23ClF3N7O4
- Peso molecular:662.02
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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
EGFR; c-Met[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.2 μM
Compound: 48
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Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31446247] |
| A549 | IC50 |
0.3 μM
Compound: 48
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Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31446247] |
| CL97 | IC50 |
0.5 μM
Compound: 48
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Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31446247] |
| CL97 | IC50 |
0.6 μM
Compound: 48
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Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31446247] |
| MDA-MB-231 | IC50 |
0.2 μM
Compound: 48
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Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31446247] |
| NCI-H1975 | IC50 |
0.3 μM
Compound: 48
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Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31446247] |
| NCI-H1975 | IC50 |
0.3 μM
Compound: 48
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Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31446247] |
| PC-9 | IC50 |
0.5 μM
Compound: 48
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Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31446247] |
| PC-9 | IC50 |
0.6 μM
Compound: 48
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Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31446247] |
EGFR-IN-8 (0-20 μM; 24-72 hours) exhibits a time- and dose-dependent inhibitory effect on the viability of A549, PC9, H1975, CL68, and CL97 cells at different time intervals, with IC50 values ranging from 0.3 to 0.6 μM and 0.2-0.5 μM after 48 and 72 h of treatment respectively[1]. EGFR-IN-8 (0-0.6 μM; 48 hours) suppresses the expression of EGFR and c-Met in these five cell lines irrespective of their mutational status[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, PC9, H1975, CL68, and CL97 cells
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Concentration:0-20 μM
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Incubation Time:24 hours, 48 hours, 72 hours
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Result:Showed inhibitory effects on different cells.
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Cell Line:A549, PC9, H1975, CL68, and CL97 cells
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Concentration:0-0.6 μM
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Incubation Time:48 hours
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Result:Decreased EGFR and c-Met expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice H1975 xenograft tumor model[1]
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Dosage:50 and 150 mg/kg
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Administration:Oral gavage; 50 and 150 mg/kg; once daily; 20 days
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Result:Inhibited H1975 xenograft tumor growth.
Chemical Information
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No. CAS 2407957-87-1
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Appearance Solid
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Peso molecular 662.02
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Fòrmula C32H23ClF3N7O4
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC(C(F)(F)F)=C(NC(C2CC2)=O)C=C1)NC3=CC=CC(C4=NC(C5=CC=C(NC(C6=CC=CN=C6)=O)C=C5Cl)=NO4)=C3
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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 : 8.33 mg/mL (12.58 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 (273 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5105 mL | 7.5526 mL | 15.1053 mL | 37.7632 mL |
| 5 mM | 0.3021 mL | 1.5105 mL | 3.0211 mL | 7.5526 mL | |
| 10 mM | 0.1511 mL | 0.7553 mL | 1.5105 mL | 3.7763 mL |
EGFR-IN-8 Related Classifications
HY-126320 Related Classifications
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