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Cat. No.: 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.

For research use only. We do not sell to patients.

CAS No.: 2890261-81-9
Formula: C₃₃H₃₇ClN₈O₃
Molecular Weight:629.15

Storage:

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

Data Sheet (273 KB)

EGFR-IN-61 Chemical Structure

CAS No.: 2890261-81-9

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Antibody-Drug Conjugates

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

EGFR^L858R/T790M

42 ± 2 nM (IC₅₀)

EGFR^{L858R/T790M/C797S}

137 ± 6 nM (IC₅₀)

EGFR (WT)

743 ± 20 nM (IC₅₀)

All EGFR Isoforms :

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.

Chemical Information

CAS No. 2890261-81-9
Molecular Weight 629.15
Formula 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 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)

References

[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]

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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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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EGFR-IN-61

All EGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGFR-IN-61 Related Classifications

HY-147860 Related Classifications