Nsc745885

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[1][2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

EZH2

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[1]. 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[1]. 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[1]. Cell Viability Assay[1] Cell Line: SAS cells is obtained from a poorly differentiated human squamous cell carcinoma Concentration: 0.5 μM, 1 μM, 1.5 μM, 2 μM, 4 μM Incubation Time: 24, 48, or 72 hours Result: Decreases SAS cells growth as a time and dose-dependent manner. Apoptosis Analysis[1] Cell Line: SAS cells is obtained from a poorly differentiated human squamous cell carcinoma Concentration: 0.5 μM, 1 μM, 1.5 μM, 2 μM, 4 μM Incubation Time: 24 hours Result: Decreases SAS cells growth as a time and dose-dependent manner. Western Blot Analysis[1] Cell Line: SAS cells is obtained from a poorly differentiated human squamous cell carcinoma Concentration: 0.5 μM, 1 μM, 1.5 μM, 2 μM Incubation Time: 24 or 48 hours Result: Increased cleaved caspase-3 expression and decreased XIAP expression.

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[1]. Animal Model: Eight-week-old NOD/SCID (NOD.CB17 Prkdcscid/J) mice[1] Dosage: 2 mg/kg Administration: Intraperitoneal injection; 2 mg/kg; once daily; 10 days Result: Inhibited engrafted tumors growth in vivo.

[1]. Chen YW, et al.A novel compound NSC745885 exerts an anti-tumor effect on tongue cancer SAS cells in vitro and in vivo.PLoS One. 2014 Aug 15;9(8):e104703.

[2]. Tang SH, et al. Pharmacologic down-regulation of EZH2 suppresses bladder cancer in vitro and in vivo.Oncotarget. 2014 Nov 15;5(21):10342-55.