BAY 2476568
Based on 1 Customer Validation
BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.88%
- CAS. Nr.: 2311901-93-4
- Formel: C24H27FN4O4
- Molecular Weight:454.49
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Alle EGFR Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
12.8 nM
Compound: BAY 2476568
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Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 48 hrs by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 48 hrs by Cell Titer-Glo assay
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[PMID: 37669428] |
| BaF3 | IC50 |
397 nM
Compound: BAY 2476568
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Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 48 hrs by Cell Titer-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 48 hrs by Cell Titer-Glo assay
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[PMID: 37669428] |
In Vitro
BAY 2476568 exhibits potent inhibitory activity against EGFR exon20 insertion mutants L858R, insASV, insSVD, and insNPG, with IC50 values of 28.3 nM, 0.09 nM, 0.21 nM, and 0.11 nM, respectively and shows no significant inhibitory activity against wild-type (WT) EGFR kinase, with an IC50 value >1000 nM[1].
BAY 2476568 (72 h) exerts potent antiproliferative activity against Ba/F3 cells expressing EGFR insASV and insSVD mutants, with IC50 values of 24 nM and 20 nM, respectively and shows weak antiproliferative activity against Ba/F3 cells expressing WT EGFR, with an IC50 value of 128 nM[1].
BAY 2476568 (100 nM, 6 h) significantly inhibits phosphorylation of EGFR (Y1068), ERK1/2, and Akt (S473) in Ba/F3 cells expressing EGFR insASV and insSVD mutants[1].
BAY 2476568 (100 nM, 6 h) only incompletely inhibits EGFR (Y1068) phosphorylation and weakly reduces ERK1/2 and Akt (S473) phosphorylation in Ba/F3 cells expressing WT EGFR[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 cells expressing EGFR insASV and insSVD mutants
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Concentration:100 nM
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Incubation Time:6 h
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Result:Inhibited phosphorylation of EGFR (Y1068), ERK1/2, and Akt (S473) in Ba/F3 cells expressing EGFR insASV and insSVD mutants.
Chemical Information
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CAS. Nr. 2311901-93-4
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Appearance Solid
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Molecular Weight 454.49
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Formel C24H27FN4O4
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Color Off-white to light yellow
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SMILES
O=C1C2=C(NC(C3=C(OCC(C)(OC)C)C=NC=C3)=C2NC4=CC=CC(F)=C4OC)CCN1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (220.03 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (279 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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Handling Instructions (2659 KB)
Verweise
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 | 2.2003 mL | 11.0013 mL | 22.0027 mL | 55.0067 mL |
| 5 mM | 0.4401 mL | 2.2003 mL | 4.4005 mL | 11.0013 mL | |
| 10 mM | 0.2200 mL | 1.1001 mL | 2.2003 mL | 5.5007 mL | |
| 15 mM | 0.1467 mL | 0.7334 mL | 1.4668 mL | 3.6671 mL | |
| 20 mM | 0.1100 mL | 0.5501 mL | 1.1001 mL | 2.7503 mL | |
| 25 mM | 0.0880 mL | 0.4401 mL | 0.8801 mL | 2.2003 mL | |
| 30 mM | 0.0733 mL | 0.3667 mL | 0.7334 mL | 1.8336 mL | |
| 40 mM | 0.0550 mL | 0.2750 mL | 0.5501 mL | 1.3752 mL | |
| 50 mM | 0.0440 mL | 0.2200 mL | 0.4401 mL | 1.1001 mL | |
| 60 mM | 0.0367 mL | 0.1834 mL | 0.3667 mL | 0.9168 mL | |
| 80 mM | 0.0275 mL | 0.1375 mL | 0.2750 mL | 0.6876 mL | |
| 100 mM | 0.0220 mL | 0.1100 mL | 0.2200 mL | 0.5501 mL |
BAY 2476568 Related Classifications
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