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NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.

NSC745885 (0.5-4 μM; 24, 48 or 72 hours) has a growth inhibitory or death-promoting effect on the SAS cells, it significantly decreases the densities of cultured cells when compared with untreated cells. The IC₅₀ of NSC745885 is 0.85 μM after 72 hours’ treatment.
NSC745885 (0.5-4 μM; 24 hours) increases annexin V positive cells in a dose-dependent manner, and the differences appears as a dose-dependent manner.
NSC745885 (0.5-2 μM; 24 or 48 hours) decreases XIAP protein levels and increases protein levels both as a dose-dependent manner in SAS cells.

NSC745885 (intraperitoneal injection; 2 mg/kg; once daily; 10 days) treatment significantly reduces tumor size when compared with the vehicle control, and exhibits a higher safety than doxorubicin.

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