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Art. -Nr.: HY-146210

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EGFR-IN-50

EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI₅₀=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI₅₀=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2044508-48-5
Formel: C₂₄H₂₆BrN₃O₄S₂
Molecular Weight:564.51

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (268 KB)

EGFR-IN-50 Chemical Structure

CAS. Nr.: 2044508-48-5

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Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	>10 μM Compound: 9h	Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 32619886]

In Vitro

EGFR-IN-50 (0-10 μM; 72 h) selectively inhibits NSCLC cell line H3255 (expressing EGFR-L858R) compared to other tumor cells^[1].
EGFR-IN-50 (1-10 μM; 72 h) induces cell cycle arrest in G0-G1 phase^[1].
EGFR-IN-50 (0.039-10 μM; 4 h) inhibits the phosphorylation of EGFR in H3255 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

A549, H3255, HepG2, MCF-7, HT-29 and A431 cells
Concentration:

0-10 μM
Incubation Time:

72 hours
Result:

Showed GI₅₀ values of >10, and 0.7873 μM for A549 and H3255 cells, respectively.
Showed IC₅₀ values of >10, 7.309, >10 and 6.703 μM for HepG2, MCF-7, HT-29 and A431 cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:

H3255 cells
Concentration:

1, 5, and 10 μM
Incubation Time:

72 hours
Result:

Increased the percentage of H3255 cells in G0-G1 phase from 60.32% to 88.61%.

Western Blot Analysis^[1]

Cell Line:

H3255 cells
Concentration:

0.039, 0.15, 0.62, 2.5, and 10 μM
Incubation Time:

4 hours
Result:

Inhibited the phosphorylation of EGFR in H3255 cells in a dose-dependent manner.

Chemical Information

CAS. Nr. 2044508-48-5
Molecular Weight 564.51
Formel C₂₄H₂₆BrN₃O₄S₂
SMILES

C=CCSSCCC(OCCCOC1=CC2=C(C(NC3=CC(Br)=CC=C3)=NC=N2)C=C1OC)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. You-Guang Zheng, et al. Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H2S) donors as potent EGFR inhibitors against L858R resistance mutation. Eur J Med Chem. 2020 Sep 15;202:112522. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biologische Aktivität
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Chemical Information
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EGFR-IN-50

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

EGFR-IN-50 Related Classifications

HY-146210 Related Classifications