2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  3. EGFR Apoptosis Akt ERK
  4. EGFR-IN-120

EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFRL858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFRWT (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 EGFRL858R/T790M/C797S with an IC50 of 0.052 μM.

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EGFR-IN-120

EGFR-IN-120 Chemical Structure

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EGFR-IN-120 Related Antibodies

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ERK ERK1 ERK2 ERK5 ERK8

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Description

EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFRL858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFRWT (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 EGFRL858R/T790M/C797S with an IC50 of 0.052 μM[1].

IC50 & Target[1]

EGFRL858R/T790M/C797S

0.053 μM (IC50)

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]
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
References
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EGFR-IN-120 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EGFR-IN-120EGFRApoptosisAktERKEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BExtracellular signal regulated kinasesEGFR mutantNSCLCInhibitorinhibitorinhibit

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