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. 2020 Dec 3;5(23):e140169. doi: 10.1172/jci.insight.140169

Figure 3. TP-0903 is active against the TKI-resistant FLT3 F691L gatekeeper mutation.

Figure 3

(A) Inhibition of viability of Ba/F3 cells expressing FLT3 mutants when treated with indicated TKI (MTT assay, 72 hours, n = 18). (B) Signaling inhibition in indicated Ba/F3 cells treated with DMSO or increasing concentrations of TP-0903 for 1 hour. Western blot analysis was performed on whole-cell lysates run on parallel gels with the indicated antibodies and is representative of 2–3 independent experiments. (C) Peripheral blood GFP+ cells following treatment TP-0903 (60 mg/kg) or gilteritinib (30 mg/kg) once daily (starting at day 3) in a Ba/F3-FLT3-ITD/F691L-GFP+ NSG mouse xenograft model (n = 3–6/cohort). GFP+ cells were measured via flow on day 15. P values were determined using 1-way ANOVA (P < 0.0001) with Tukey multiple comparison test, with specific P values indicated within the figure.