Figure 1.
Characterization of eftoza single-agent activity in human AML cell lines. (A) AML cell lines were treated with eftoza for 24 hours and the impact on cell viability was determined using CellTiter-Glo. Half maximal effective concentration (EC50) values were calculated from the resulting dose-response curves using GraphPad Prism. Data represent the mean ± standard error of the mean (SEM; n = ≥3). The TP53 status of AML cell lines (supplemental Table 3) was obtained from the World Health Organization International Agency for Research on Cancer. Red bars depict cell lines expressing TP53 wild-type (TP53wt); green bars depict cell lines harboring mutations affecting the expression of TP53 (TP53mut). (B) OCI-AML2 and SKM-1 cells were treated with eftoza for 24 hours and the impact on caspase-3/7 activity was determined in relation to cell viability using Caspase-Glo 3/7 and CellTiter-Glo, respectively. Data represent the mean ± SEM (n = 3). (C) Dose-response curves of OCI-AML2 and SKM-1 cell lines treated with eftoza for 24 hours alone or pretreated 1 hour with z-VAD-FMK (zvad). Viability was determined using CellTiter-Glo. Data represent the mean ± SEM (n = 3). (D) Mice bearing SKM-1 tumors were treated with eftoza (1 mg/kg, every other day × 5) administered intraperitoneally, and the effect on tumor volumes was determined. Data represent the mean ± SEM of 8 mice per treatment group. (E-F) DR4 (E) and DR5 (F) plasma membrane receptor number was determined in a panel of AML cell lines via quantitative flow cytometry. Data represent the mean ± SEM (n ≥2). (G,H) The plasma membrane expression of DR4, DR5, and total DRs (DR4 + DR5) was measured via flow cytometry in the panel of AML cell lines and the correlation with eftoza EC50 values from panel A was determined. The statistical significance was determined using Spearman correlation. (I) Parental and +huDR4- and +huDR5-overexpressing HEL cells were treated with eftoza for 24 hours and the impact on cell viability was determined using CellTiter-Glo. Data represent the mean ± standard deviation (n = 3). Numbers in brackets indicate the mean DR4 or DR5 plasma membrane receptor numbers (mean ± SEM; n = 3).

Characterization of eftoza single-agent activity in human AML cell lines. (A) AML cell lines were treated with eftoza for 24 hours and the impact on cell viability was determined using CellTiter-Glo. Half maximal effective concentration (EC50) values were calculated from the resulting dose-response curves using GraphPad Prism. Data represent the mean ± standard error of the mean (SEM; n = ≥3). The TP53 status of AML cell lines (supplemental Table 3) was obtained from the World Health Organization International Agency for Research on Cancer. Red bars depict cell lines expressing TP53 wild-type (TP53wt); green bars depict cell lines harboring mutations affecting the expression of TP53 (TP53mut). (B) OCI-AML2 and SKM-1 cells were treated with eftoza for 24 hours and the impact on caspase-3/7 activity was determined in relation to cell viability using Caspase-Glo 3/7 and CellTiter-Glo, respectively. Data represent the mean ± SEM (n = 3). (C) Dose-response curves of OCI-AML2 and SKM-1 cell lines treated with eftoza for 24 hours alone or pretreated 1 hour with z-VAD-FMK (zvad). Viability was determined using CellTiter-Glo. Data represent the mean ± SEM (n = 3). (D) Mice bearing SKM-1 tumors were treated with eftoza (1 mg/kg, every other day × 5) administered intraperitoneally, and the effect on tumor volumes was determined. Data represent the mean ± SEM of 8 mice per treatment group. (E-F) DR4 (E) and DR5 (F) plasma membrane receptor number was determined in a panel of AML cell lines via quantitative flow cytometry. Data represent the mean ± SEM (n ≥2). (G,H) The plasma membrane expression of DR4, DR5, and total DRs (DR4 + DR5) was measured via flow cytometry in the panel of AML cell lines and the correlation with eftoza EC50 values from panel A was determined. The statistical significance was determined using Spearman correlation. (I) Parental and +huDR4- and +huDR5-overexpressing HEL cells were treated with eftoza for 24 hours and the impact on cell viability was determined using CellTiter-Glo. Data represent the mean ± standard deviation (n = 3). Numbers in brackets indicate the mean DR4 or DR5 plasma membrane receptor numbers (mean ± SEM; n = 3).

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