EGFR-IN-201
EGFR-IN-201 is a potent EGFR inhibitor, with an IC50 of 0.091 μM against wild-type EGFR; for mutant EGFR variants, the IC50 values of EGFRT790M, EGFRL858R and EGFRC797S are 0.147 μM, 0.221 μM and 0.703 μM, respectively. EGFR-IN-201 inhibits EGFR downstream signaling proteins AKT1 (IC50 = 0.225 μg/mL) and ERK1 (IC50 = 0.705 μg/mL). EGFR-IN-201 induces G0/G1 cell cycle arrest, apoptosis and low-level necrosis in cancer cells. EGFR-IN-201 is applicable to research on cancers such as colon cancer.
For research use only. We do not sell to patients.
- CAS No.: 3103654-99-2
- Formula: C17H16N4O2S
- Molecular Weight:340.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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EGFR (WT) 0.091 μM () |
EGFRT790M 0.147 μM () |
EGFRL858R 0.221 μM () |
EGFRC797S 0.703 μM () |
ERK1 0.705 μg/mL () |
Akt1 0.225 μg/mL () |
Caspase-3 |
Caspase-9 |
Bax |
Bcl-2 |
EGFR-IN-201 (Compound 5c) (0.01-100 μM) inhibits the growth of NCI-60 cancer cell lines with GI50 values of 2.77-20.70 μM, showing potent activity against multiple solid and hematologic tumor types[1].
EGFR-IN-201 (Compound 5c) (IC50 concentration) induces G0/G1 phase cell cycle arrest in HT-29 human colon adenocarcinoma cells[1].
EGFR-IN-201 (Compound 5c) (IC50 concentration) potently induces apoptosis (26.51% total) and moderately increases necrosis in HT-29 human colon adenocarcinoma cells[1].
EGFR-IN-201 (Compound 5c) (IC50 concentration) modulates apoptosis-related gene expression in HT-29 cells by upregulating caspase-3, caspase-9, and Bax, and downregulating Bcl-2, increasing the Bax/Bcl-2 ratio by 14.1-fold[1].
EGFR-IN-201 (Compound 5c) (range; to determine IC50) shows low cytotoxicity against normal human lung fibroblast WI-38 cells, with an IC50 of 51.903 μM, indicating a favorable safety profile relative to cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3103654-99-2
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Molecular Weight 340.40
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Formula C17H16N4O2S
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SMILES
COC1=CC=C(/C=C2C(N/C(S/2)=N\N=C(C)\C3=CC=CN3)=O)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
EGFR-IN-201 Related Classifications
HY-181659 Related Classifications
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