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Art. -Nr.: HY-153605

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EGFR-IN-77

EGFR-IN-77 (Compound 4a) is a selective EGFR^T790M/L858R inhibitor, with an IC₅₀ of 0.101 μM against EGFR^T790M/L858R, 0.477 μM against EGFR^L858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFR^T790M/L858R non-small cell lung cancer. EGFR-IN-77 can be used for the research of EGFR^L858R/T790M double-mutant non-small cell lung cancer.

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CAS. Nr.: 2222930-49-4
Formel: C₂₆H₂₈N₆O₃
Molecular Weight:472.54

Speicherung:

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

EGFR-IN-77 Chemical Structure

CAS. Nr.: 2222930-49-4

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Antibody-Drug Conjugates

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
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Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EGFR^L858R/T790M

0.101 μM (IC₅₀)

EGFR^L858R

0.477 μM (IC₅₀)

EGFR^WT

1.771 μM (IC₅₀)

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H1975	IC₅₀	0.184 μM Compound: 4a	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
NCI-H292	IC₅₀	8.321 μM Compound: 4a	Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
PC-9	IC₅₀	0.137 μM Compound: 4a	Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]

In Vitro

EGFR-IN-77 inhibits purified TL double mutant EGFR kinase with an IC₅₀ of 0.101 μM, L858R mutant EGFR kinase with an IC₅₀ of 0.477 μM, and WT EGFR kinase with an IC₅₀ of 1.771 μM, exhibiting 17.52-fold selectivity for TL EGFR over WT EGFR^[1].
EGFR-IN-77 inhibits proliferation of H1975 (TL EGFR) NSCLC cells with an IC₅₀ of 0.184 μM, PC9 (L858R EGFR) cells with an IC₅₀ of 0.137 μM, and H292 (WT EGFR) cells with an IC₅₀ of 8.321 μM, exhibiting 45.27-fold selectivity for H1975 cells over H292 cells^[1].

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

Chemical Information

CAS. Nr. 2222930-49-4
Molecular Weight 472.54
Formel C₂₆H₂₈N₆O₃
SMILES

O=C(NC1=CC(NC2=NC(C3=CN(C)C4=C3C=CC=C4)=CC=N2)=C(C=C1N(CCO)C)OC)C=C
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

Handling Instructions (2659 KB)

Verweise

[1]. An B, et al. The discovery of a potent and selective third-generation EGFR kinase inhibitor as a therapy for EGFR L858R/T790M double mutant non-small cell lung cancer. Eur J Med Chem. 2019 Dec 1;183:111709. [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.

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
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EGFR-IN-77

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

EGFR-IN-77 Related Classifications

HY-153605 Related Classifications