Fig. 3 | Signal Transduction and Targeted Therapy

Fig. 3

From: Potent and selective LSD1 inhibitor DC551040 reveals a promising combination therapy for AML with insight into epigenetic dysregulation

Fig. 3The alternative text for this image may have been generated using AI.

DC551040 has an antitumor effect in acute myeloid leukemia in vivo. a, b DC551040 anti-tumor effect in Kasumi-1 xenografts. The relative tumor volume (RTV) was calculated twice weekly; tumors were excised and measured at study end. Mice was treated with DC551040 (0.5/1/2 mg/kg/day), GSK2879552 (2 mg/kg/day), or vehicle (treatment duration: 17 days). Data: mean ± SEM, n = 6/group. c, d DC551040 anti-tumor effect in MV-4-11 xenografts. RTV was calculated twice weekly; tumors were excised and measured at study end. Mice was treated with DC551040 (5/10 mg/kg/day), GSK2879552 (10 mg/kg/day), or vehicle (treatment duration: 22 days). Data: mean ± SEM, n = 6/group. e, f DC551040-induced CD86 upregulation in MV-4-11 xenografts (immunohistochemistry). Mice treated with DC551040 (5/10 mg/kg/day), GSK2879552 (10 mg/kg/day), or vehicle. Data: mean ± SEM, n = 6/group. g The anti-cancer effect of DC551040 on MV-4-11 disseminated xenograft mice model. Survival for randomized mice bearing MV-4-11 tumors treated with 0.5, 2, and 4 mg/kg/day DC551040, 0.5 mg/kg/day GSK2879552, and vehicle group. Drug treatment started from recording the survival time and lasted for 21 days, n = 10 per group. h Anti-tumor effect of DC551040 ± Cytarabine (AraC) in MV-4-11 xenografts. RTV was calculated twice weekly; tumors were excised and measured at study end. Mice was treated with DC551040 (2/5 mg/kg/day), AraC (20 mg/kg/day), DC551040+AraC, or vehicle (treatment duration: 22 days). Data: mean ± SEM, n = 6/group. i The anti-cancer effect of DC551040, Cytarabine and Daunorubicin on MV-4-11 disseminated xenograft mice model. Survival for randomized mice bearing MV-4-11 tumors treated with 0.5 mg/kg/day DC551040, 7.5 mg/kg/day AraC and 0.75 mg/kg/day DAC, DC551040 + AraC + DAC, and vehicle group. Drug treatment started from recording the survival time and lasted for 21 days, n = 10 per group. The Significance of (a, b, c, d, f, h) was analyzed by equal variance two-tailed t test. The Significance of (g, i) was analyzed by logrank test. *P < 0.05, **P < 0.01, ***P < 0.001

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