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Art. -Nr.: HY-147860

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EGFR-IN-61

EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC₅₀ values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC₅₀ values of 2.14 and 1.82 μM, respectively.

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CAS. Nr.: 2890261-81-9
Formel: C₃₃H₃₇ClN₈O₃
Molecular Weight:629.15

Speicherung:

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

Data Sheet (273 KB)

EGFR-IN-61 Chemical Structure

CAS. Nr.: 2890261-81-9

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Protokoll (2)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EGFR^L858R/T790M

42 ± 2 nM (IC₅₀)

EGFR^{L858R/T790M/C797S}

137 ± 6 nM (IC₅₀)

EGFR (WT)

743 ± 20 nM (IC₅₀)

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.14 μM Compound: 22a	Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 35696862]
A549	IC₅₀	2.14 μM Compound: 150	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38879996]
NCI-H1975	IC₅₀	1.82 μM Compound: 22a	Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 35696862]
NCI-H1975	IC₅₀	1.82 μM Compound: 150	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38879996]

In Vitro

EGFR-IN-61 (compound 22a) shows excellent kinase selectivity against the L858R/T790M/C797S mutant EGFR kinase rather than the wild-type, which reached 5.4 times^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Chemical Information

CAS. Nr. 2890261-81-9
Molecular Weight 629.15
Formel C₃₃H₃₇ClN₈O₃
SMILES

COC1=CC(N(CCN(C)C)C)=C(C=C1NC2=NC(C3=CN(C4=C3C=CC=C4)CCCO)=CC=N2)NC(C5=CC(Cl)=NC=C5)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Protokoll

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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]. Ding S, et al. Design, synthesis and biological evaluation of novel osimertinib derivatives as reversible EGFR kinase inhibitors. Eur J Med Chem. 2022 Aug 5;238:114492. [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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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