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 EGFR^T790M, EGFR^L858R and EGFR^C797S 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^[1].

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.

340.40

C₁₇H₁₆N₄O₂S

3103654-99-2

COC1=CC=C(/C=C2C(N/C(S/2)=N\N=C(C)\C3=CC=CN3)=O)C=C1

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• [1]. Elsisi WI, et al. Targeting EGFR with thiazolidin-4-ones: Structure-guided design, synthesis, and in silico profiling for anticancer drug discovery. Eur J Med Chem. 2025;300:118142.  [Content Brief]