TrxR/EGFR-IN-1
TrxR/EGFR-IN-1 is a TrxR/GFR inhibitor and a Gefitinib (HY-50895) derivative. TrxR/EGFR-IN-1 inhibits TrxR and EGFR, downregulates p‑EGFR, p‑AKT, and p‑ERK; promotes GPX4 protein degradation through dual autophagy-lysosomal and proteasomal pathways, triggering ferroptosis. TrxR/EGFR-IN-1 induces endoplasmic reticulum stress, immunogenic cell death, and apoptosis, increasing intracellular ROS and oxidative stress. TrxR/EGFR-IN-1 exhibits in vitro antiproliferative activity against both Gefitinib-sensitive and Gefitinib-resistant non-small cell lung cancer. TrxR/EGFR-IN-1 inhibits tumor growth in the PC9GR xenograft tumor model. TrxR/EGFR-IN-1 can be used for lung cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 3038386-42-1
- Formula: C24H24AuClFN6O2P
- Molecular Weight:710.88
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
EGFR |
Akt |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| PC-9 | IC50 |
0.012 μM
|
Antiproliferative activity against human PC9 lung adenocarcinoma cells assessed as viability reduction after 72 hrs incubation by CCK-8 assay.
Antiproliferative activity against human PC9 lung adenocarcinoma cells assessed as viability reduction after 72 hrs incubation by CCK-8 assay.
|
39968846 |
| H1975 | IC50 |
1.84 μM
|
Antiproliferative activity against human H1975 lung adenocarcinoma cells assessed as viability reduction after 72 hrs incubation by CCK-8 assay.
Antiproliferative activity against human H1975 lung adenocarcinoma cells assessed as viability reduction after 72 hrs incubation by CCK-8 assay.
|
39968846 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:PC9, PC9GR, and H1975 human lung adenocarcinoma cells
-
Concentration:0.1, 0.5 μM (PC9)
4, 8 μM (PC9GR)
2, 4 μM (H1975) -
Incubation Time:0, 12, 24, 36, 48, 60, 72 h
-
Result:Inhibited proliferation of PC9, PC9GR, and H1975 cells with IC50 values of 0.012, 1.76, and 1.84 μM, respectively.
-
Cell Line:PC9, PC9GR, and H1975 human lung adenocarcinoma cells
-
Concentration:0.1, 0.5 μM (PC9)
4, 8 μM (PC9GR)
2, 4 μM (H1975) -
Incubation Time:48 h
-
Result:Induced apoptosis in PC9, PC9GR, and H1975 cells.
-
Cell Line:PC9, PC9GR, and H1975 human lung adenocarcinoma cells
-
Concentration:0.1, 0.5 μM (PC9)
4, 8 μM (PC9GR)
2, 4 μM (H1975) -
Incubation Time:48 h
-
Result:Inhibited migration in PC9, PC9GR, and H1975 cells.
-
Cell Line:PC9, PC9GR, and H1975 human lung adenocarcinoma cells
-
Concentration:0.1, 0.5 μM (PC9)
4, 8 μM (PC9GR)
2, 4 μM (H1975) -
Incubation Time:2 weeks
-
Result:Inhibited colony formation in PC9, PC9GR, and H1975 cells.
-
Cell Line:PC9, PC9GR, and H1975 human lung adenocarcinoma cells
-
Concentration:0, 0.01, 0.05 μM (PC9)
0, 4, 8 μM (PC9GR)
0, 2, 4 μM (H1975) -
Incubation Time:48 h
-
Result:In PC9 cells, 0.05 μM L1Au2 inhibited activation of the EGFR-related pathway.
In PC9GR cells, L1Au2 inhibited EGFR phosphorylation and effectively inhibited AKT and ERK phosphorylation and total protein levels.
In H1975 cells, L1Au2 inhibited EGFR phosphorylation more weakly than gefitinib but effectively inhibited AKT and ERK phosphorylation and total protein levels.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c-nude (female, 4 weeks old, PC9GR cells (3 × 106))[1]
-
Dosage:10 mg/kg
-
Administration:i.p.; twice every 3 days; days 10, 12, 13, 15, 16, 18, 19, 21, 22, and 24
-
Result:Reduced growth of gefitinib-resistant PC9GR subcutaneous tumors; effect was superior to gefitinib.
Decreased GPX4 expression in subcutaneous tumor tissues and increased DHE and 4-HNE levels in subcutaneous tumor tissues.
Inhibited TrxR activity in subcutaneous tumor tissues.
Inhibited EGFR phosphorylation in subcutaneous tumor tissues.
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Autophagy
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Ferroptosis Solutions
- Lysosome and acidic-vesicle live-cell staining
- Subcutaneous Cell-Line-Derived Xenograft
- Macroautophagy Solutions
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
-
CAS No. 3038386-42-1
-
Molecular Weight 710.88
-
Formula C24H24AuClFN6O2P
-
SMILES
ClC1=C(F)C=CC(NC2=NC=NC3=C2C=C(OCC#C[Au][P]45CN6CN(CN(C6)C5)C4)C(OC)=C3)=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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)