Antitumor agent-218 

Antitumor agent-218 is an aggregation-induced emission (AIE)-based photosensitizer. Antitumor agent-218 selectively accumulates in the endoplasmic reticulum, and generates ROS within the endoplasmic reticulum upon irradiation to induce necroptosis of tumor cells. Antitumor agent-218 can be used in cancer-related research^[1].

Antitumor agent-218 (Compound A04) (0.63-100 μM; 48 h) potently inhibits the viability of 4T1 cells via phototoxicity, with an IC₅₀ value of 0.63 μM; meanwhile, this compound exhibits negligible dark toxicity (CC₅₀ > 100 μM), with a selectivity index >158.7^[1].
Antitumor agent-218 (0.61-100 μM; 48 h) potently inhibits the viability of HeLa cells via phototoxicity, with an IC₅₀ of 0.61 μM, while exhibiting negligible dark toxicity (CC₅₀ > 100 μM) and a selectivity index > 163.9^[1].
Antitumor agent-218 (5 μM; 6 h) efficiently induces the production of intracellular reactive oxygen species (ROS) in 4T1 cells under white light irradiation^[1].
Antitumor agent-218 (5 μM; 1-6 h) is taken up by 4T1 cells in a time-dependent manner, with a gradual increase in intracellular fluorescence intensity observed at 1, 3, and 6 h of incubation^[1].
Antitumor agent-218 (5 μM; 3 h) selectively accumulates in the endoplasmic reticulum of 4T1 cells, with a Pearson correlation coefficient of 0.91 with ER-Tracker Green^[1].
Photodynamic therapy mediated by Antitumor agent-218 (0.6 μM; 52-56 h) induces necroptosis in 4T1 cells, which is evidenced by the restoration of cell viability by Nec-1, increased phosphorylation level of MLKL, and upregulated expression of necroptosis-related genes MLKL, RIPK1 and RIPK3^[1].
The phototoxicity of 4T1 cells mediated by Antitumor agent-218 (10 μM) is oxygen-independent, with comparable decreases in cell viability (approximately 15% at 10 μM) observed under normoxic (21% O₂) and hypoxic (5% O₂) conditions^[1].

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

534.65

C₃₆H₃₀N₄O

3094774-72-5

CC1=CC=C(C=C1)N(C2=CC=C(C=C2)/C=C/C3=C/C(C4=CC=CC=C4N3CCO)=C(C#N)/C#N)C5=CC=C(C=C5)C

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• [1]. Fang L, et al. Peripheral structural engineering of quinoline-malononitrile-triphenylamine (QM-TPA) core enhances Anti-tumor PDT efficacy through necroptosis. Eur J Med Chem. Published online May 14, 2026.