2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  3. EGFR PI3K Akt Reactive Oxygen Species (ROS) Caspase
  4. EGFR-IN-214

EGFR-IN-214 is an orally active EGFR inhibitor with an EC50 of 3.353 μM. EGFR-IN-214 blocks the downstream PI3K/Akt signaling pathway, induces intracellular ROS accumulation and Caspase-dependent apoptosis. EGFR-IN-214 exhibits antiproliferative activity in cancer cells and inhibits tumor growth in xenograft models. EGFR-IN-214 can be used in studies related to hepatocellular carcinoma.

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EGFR-IN-214

EGFR-IN-214 Chemical Structure

CAS No. : 3077316-17-4

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EGFR-IN-214 Related Antibodies

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

EGFR-IN-214 is an orally active EGFR inhibitor with an EC50 of 3.353 μM. EGFR-IN-214 blocks the downstream PI3K/Akt signaling pathway, induces intracellular ROS accumulation and Caspase-dependent apoptosis. EGFR-IN-214 exhibits antiproliferative activity in cancer cells and inhibits tumor growth in xenograft models. EGFR-IN-214 can be used in studies related to hepatocellular carcinoma[1].

In Vitro

EGFR-IN-214 (0.5-4 μM; 72 h) potently inhibits the viability of HepG2 (IC50 = 2.20 μM) and Huh7 (IC50 = 1.16 μM) human hepatocellular carcinoma cells in vitro[1].
EGFR-IN-214 (0.05-0.4 μM; continuous incubation for colony formation) potently suppresses the colony-forming ability of HepG2 and Huh7 human hepatocellular carcinoma cells in a concentration-dependent manner[1].
EGFR-IN-214 (0.5-4 μM; 72 h) induces caspase-dependent mitochondrial apoptosis in HepG2 and Huh7 human hepatocellular carcinoma cells in vitro in a concentration-dependent manner[1].
EGFR-IN-214 (0.5-4 μM; 72 h) disrupts mitochondrial redox homeostasis by inducing robust concentration-dependent accumulation of intracellular ROS and mitochondrial superoxide in HepG2 and Huh7 human hepatocellular carcinoma cells[1].
EGFR-IN-214 (0.5-4 μM; 72 h) suppresses the EGFR/PI3K/Akt signaling pathway in HepG2 and Huh7 human hepatocellular carcinoma cells by reducing EGFR phosphorylation and total EGFR levels, leading to downstream inhibition of PI3K and AKT phosphorylation[1].

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

EGFR-IN-214 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HepG2 and Huh7 cells
Concentration: 0.5, 1 and 2 μM (Huh7 cells); 1, 2 and 4 μM (HepG2 cells)
Incubation Time: 72 h
Result: Induced caspase-dependent mitochondrial apoptosis.

Western Blot Analysis[1]

Cell Line: HepG2 and Huh7 cells
Concentration: 0.5, 1 and 2 μM (Huh7 cells); 1, 2 and 4 μM (HepG2 cells)
Incubation Time: 72 h
Result: Increased Bax, Cleaved Caspase-3.
Reduced Bcl-2, p-EGFR/Total EGFR, p-PI3K/p-Akt and p-ERK.
Parmacokinetics
Species Dose Route T1/2 Vss CL AUC
Rat[1] 10 mg/kg i.v. 13.46 h 167.36 L/kg 0.15 L/min/kg 69.5 mg/min/L
In Vivo

EGFR-IN-214 (Compound 3b) (15-30 mg/kg; i.g.; every other day; 14 days) exhibits potent, dose-dependent antitumor activity in a Huh7 hepatocellular carcinoma xenograft model, significantly reducing tumor growth[1].

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

Animal Model: BALB/c nude (male, 5 weeks old, subcutaneously inoculated with 5×106 Huh7 cells)[1]
Dosage: 15 mg/kg; 30 mg/kg
Administration: i.g.; every other day; 14 days
Result: Showed potent, dose-dependent tumor growth suppression compared to vehicle control.
Demonstrated improved antitumor efficacy relative to positive control Icaritin at 30 mg/kg.
Significantly reduced EGFR-positive area and Ki67-positive area in tumor tissues.
Maintained stable body weight throughout the study.
Caused no obvious histopathological abnormalities in major organs (heart, liver, spleen, lung, kidney) and organ indices comparable to control.
Molecular Weight

766.71

Formula

C39H37F3N2O11
CAS No.
SMILES

O=C1C(O[C@H]2[C@H](O)[C@H](O)[C@@H](O)[C@H](C)O2)=C(C3=CC=C(OC)C=C3)OC4=C1C(O)=CC(OCC5=NN=C(/C=C/C6=CC=C(C(F)(F)F)C=C6)O5)=C4C/C=C(C)\C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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EGFR-IN-214 Related Classifications

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  • 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-2143077316-17-4EGFRPI3KAktReactive Oxygen Species (ROS)CaspaseEpidermal growth factor receptorErbB-1HER1Phosphoinositide 3-kinasePKBProtein kinase Bhepatocellular carcinomaxenograft modelsPI3K/Akt signalingHepG2reactive oxygen speciesmitochondrial apoptosiscaspase-dependent apoptosisHuh7mitochondrial superoxideInhibitorinhibitorinhibit

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