2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Apoptosis
  3. EGFR PI3K Akt Apoptosis
  4. EGFR-IN-213

EGFR-IN-213 is a selective inhibitor of EGFRL858R/T790M/C797S with a human IC50 of 0.48 nM. EGFR-IN-213 acts as an antiproliferative agent, inducing apoptosis and cell cycle arrest, and inhibiting colony formation, cell migration, and tube formation. EGFR-IN-213 can be used for the research of non-small cell lung cancer, chronic myeloid leukemia, gastric cancer, prostate cancer.

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

EGFR-IN-213

EGFR-IN-213 Chemical Structure

CAS No. : 3115216-45-7

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EGFR-IN-213 Related Antibodies

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Description

EGFR-IN-213 is a selective inhibitor of EGFRL858R/T790M/C797S with a human IC50 of 0.48 nM. EGFR-IN-213 acts as an antiproliferative agent, inducing apoptosis and cell cycle arrest, and inhibiting colony formation, cell migration, and tube formation. EGFR-IN-213 can be used for the research of non-small cell lung cancer, chronic myeloid leukemia, gastric cancer, prostate cancer[1].

IC50 & Target[1]

EGFRL858R/T790M/C797S

0.48 nM (IC50)

Akt

 

PI3K

 

In Vitro

EGFR-IN-213 (compound 8c) (1 h) potently and selectively inhibits EGFRL858R/T790M/C797S kinase with an IC50 of 0.48 nM[1].
EGFR-IN-213 (72 h) potently inhibits the proliferation of BaF3-EGFRL858R/T790M/C797S cells (IC50 = 0.249 μM) and H1975 cells (IC50 = 0.082 μM), while showing reduced activity against non-target cancer cell lines and negligible toxicity to HEK-293T cells[1].
EGFR-IN-213 (0.3-1 μM; 24 h) concentration-dependently arrests BaF3-EGFRL858R/T790M/C797S cells in the G1 phase, with stronger activity than Brigatinib (HY-12857) at 0.3 μM and 1 μM[1].
EGFR-IN-213 (1-9 μM; 48 h) concentration-dependently induces apoptosis in BaF3-EGFRL858R/T790M/C797S cells, with stronger activity than Brigatinib at 1 μM, 3 μM, and 9 μM[1].
EGFR-IN-213 (0.3-3 μM; 48 h) concentration-dependently induces apoptotic morphological changes in H1975 cells[1].
EGFR-IN-213 (1-3 μM (BaF3-EGFRL858R/T790M/C797S cells); 0.3-1 μM (H1975 cells); 24 h) concentration-dependently inhibits EGFR phosphorylation in BaF3-EGFRL858R/T790M/C797S cells, and suppresses EGFR, PI3K, and AKT phosphorylation in H1975 cells, with greater potency and selectivity than Brigatinib[1].
EGFR-IN-213 (1-3 μM; 24 h) concentration-dependently inhibits colony formation by H1975 cells[1].
EGFR-IN-213 (0.1-1 μM (Transwell migration); 1 μM (wound healing); 24 h (Transwell migration); 48 h (wound healing)) dose-dependently inhibits the migratory capacity of H1975 cells in both Transwell and wound healing assays[1].
EGFR-IN-213 (0.3-3 μM; 48 h) concentration-dependently inhibits tube formation by HUVECs, demonstrating anti-angiogenic activity[1].

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

EGFR-IN-213 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: BaF3-EGFR(L858R/T790 M/C797S) cells
Concentration: 0.3, 1 μM
Incubation Time: 24 h
Result: Induced G1 phase arrest in 83.43% of BaF3-EGFR(L858R/T790 M/C797S) cells at 0.3 μM.
Induced G1 phase arrest in 88.97% of BaF3-EGFR(L858R/T790 M/C797S) cells at 1 μM.
Showed superior activity compared to brigatinib at equivalent concentrations.

Apoptosis Analysis[1]

Cell Line: BaF3-EGFR(L858R/T790 M/C797S) cells
Concentration: 1, 3, 9 μM
Incubation Time: 48 h
Result: Induced apoptosis in 79.54% of BaF3-EGFR(L858R/T790 M/C797S) cells at 1 μM.
Induced apoptosis in 89.60% of BaF3-EGFR(L858R/T790 M/C797S) cells at 3 μM.
Induced apoptosis in 97.08% of BaF3-EGFR(L858R/T790 M/C797S) cells at 9 μM.
Showed greater pro-apoptotic activity than brigatinib at equivalent concentrations.

Apoptosis Analysis[1]

Cell Line: H1975 cells
Concentration: 0.3, 1, 3 μM
Incubation Time: 48 h
Result: Induced apoptotic morphological changes including yellow-green (early apoptosis) and orange-red (late apoptosis) fluorescence with AO/EB staining in a concentration-dependent manner.
Induced nuclear shrinkage, fragmentation, and enhanced fluorescence intensity with Hoechst33342 staining in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: BaF3-EGFR(L858R/T790 M/C797S) and H1975 cells
Concentration: 1, 3 μM (BaF3-EGFR(L858R/T790 M/C797S) cells); 0.3, 1 μM (H1975 cells)
Incubation Time: 24 h
Result: Concentration-dependently suppressed EGFR phosphorylation in BaF3-EGFR(L858R/T790 M/C797S) cells, with greater potency than brigatinib.
Dose-dependently suppressed phosphorylation of EGFR, PI3K, and AKT in H1975 cells, with greater selectivity for EGFR phosphorylation inhibition than brigatinib.

Cell Proliferation Assay[1]

Cell Line: H1975 cells
Concentration: 1, 3 μM
Incubation Time: 24 h
Result: Decreased the number of H1975 cell colonies in a concentration-dependent manner, with fewer colonies observed at higher concentrations.

Cell Invasion Assay[1]

Cell Line: H1975 cells
Concentration: 0.1, 0.3, 1 μM (Transwell migration); 1 μM (wound healing)
Incubation Time: 24 h (Transwell migration); 24, 48 h (wound healing)
Result: Dose-dependently reduced the number of migrated H1975 cells in the Transwell assay, with similar inhibitory effect to brigatinib.
Markedly impeded wound closure in the wound healing assay at 1 μM compared to the control group, with similar activity to brigatinib.
Molecular Weight

759.11

Formula

C35H43Cl3N9O2P
CAS No.
SMILES

CP(C)(C1=CC=CC=C1NC2=NC(NC3=CC(NCC4=C(Cl)C(Cl)=NC=C4)=C(N5CCC(N6CCN(C)CC6)CC5)C=C3OC)=NC=C2Cl)=O
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Purity & Documentation
References
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EGFR-IN-213 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-2133115216-45-7EGFRPI3KAktApoptosisEpidermal growth factor receptorErbB-1HER1Phosphoinositide 3-kinasePKBProtein kinase Bgastric cancernon-small cell lung cancerEGFR (L858R/T790M/C797S mutant)H1975 cellsBaF3-EGFR(L858R/T790 M/C797S) cellsHUVECsapoptosisprostate cancerHEK-293T cellschronic myeloid leukemiaInhibitorinhibitorinhibit

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