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.
For research use only. We do not sell to patients.
- CAS No.: 3094774-72-5
- Formula: C36H30N4O
- Molecular Weight:534.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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.
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Cell Line:4T1 cells
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Concentration:0.6 μM
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Incubation Time:24 h (co-incubation); 10 min (light irradiation); 24 h (post-irradiation incubation); 4 h, 8 h (qRT-PCR measurements post-irradiation)
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Result:Restored 4T1 cell viability by more than 50% when co-incubated with necroptosis inhibitor Nec-1, while inhibitors of apoptosis, autophagy, and ferroptosis showed no significant effect on viability.
Induced time-dependent phosphorylation of MLKL detected via immunoblot analysis.
Upregulated necroptosis-related genes (MLKL, RIPK1, RIPK3) at 4 h and 8 h post-irradiation detected via qRT-PCR.
Chemical Information
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CAS No. 3094774-72-5
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Molecular Weight 534.65
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Formula C36H30N4O
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SMILES
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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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)