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. 2021 Jan 28;106(4):1022–1033. doi: 10.3324/haematol.2020.247346

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Copyright© 2021 Ferrata Storti Foundation

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Figure 3. — Plasma inhibitory activity (PIA) assays for MYC. (A) PIA assays for MYC were performed on patients' plasma samples collected at different time points throughout cycle 1 day 1 in a dose escalation study of PLX51107. Out of six cohorts, only the samples from the four cohorts receiving the highest doses exhibited MYC suppression in the MYC surrogate assay (shown here). Cohorts 5 and 6, receiving 120 mg or 160 mg of PLX51107 per day, produced the maximal MYC suppressive effect, which lasted for approximately 6 hours (h). (B) A total of 17 patients’ plasma sets were analyzed by the PIA assay. Each symbol represents a time point for a particular patient. The MYC PIA result for each point is plotted against the concentration of PLX51107 measured in that sample. The plasma standard curve (solid black line) was generated from OCI-AML3 dose responses in Figure 1A. (C) PIA assays for cohort 5 are plotted against time after dosing. Values for MYC expression were obtained through densitometry and the 6-h length of MYC suppression is indicated by the bracket.