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Cat. No.: HY-161923

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EGFR-IN-120

EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFR^{L858R/T790M/C797S} with an IC₅₀ value of 0.053 μM, and has a relatively weak effect on EGFR^WT (IC₅₀: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cell apoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFR^{L858R/T790M/C797S} with an IC₅₀ of 0.052 μM.

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

Formula: C₃₁H₃₅FN₈O₂
Molecular Weight:570.66

Storage:

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

Data Sheet (273 KB)

EGFR-IN-120 Chemical Structure

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

EGFR^{L858R/T790M/C797S}

0.053 μM (IC₅₀)

All EGFR Isoforms :

All Akt Isoforms :

All ERK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	1.067 μM Compound: 11eg	Cytotoxicity against human A-431 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human A-431 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
HCC827	IC₅₀	0.108 μM Compound: 11eg	Cytotoxicity against human HCC827 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human HCC827 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
MCF7	IC₅₀	3.61 μM Compound: 11eg	Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
NCI-H1975	IC₅₀	0.106 μM Compound: 11eg	Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
PC-9	IC₅₀	0.052 μM Compound: 11eg	Cytotoxicity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
PC-9	IC₅₀	0.144 μM Compound: 11eg	Cytotoxicity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]
PC-9	IC₅₀	0.201 μM Compound: 11eg	Cytotoxicity against human PC-9 cells expressing EGFR Del19/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against human PC-9 cells expressing EGFR Del19/T790M/C797S mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39094277]

Chemical Information

Molecular Weight 570.66
Formula C₃₁H₃₅FN₈O₂
SMILES

FC1=C(C2=CC=C(C=C(C(NC)=O)N3C(C)C)C3=C2)N=C(NC4=CC=C(N5CCN(C)CC5)C(NC(C=C)=O)=C4)N=C1
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]. Wang X, et al. Novel EGFR inhibitors against resistant L858R/T790M/C797S mutant for intervention of non-small cell lung cancer. Eur J Med Chem. 2024 Jul 26;277:116711. [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.

Keywords

100 mg

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

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EGFR-IN-120

All EGFR Isoforms

All Akt Isoforms

All ERK Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGFR-IN-120 Related Classifications

HY-161923 Related Classifications