Bisantrene

Bisantrene is an inhibitor of fat mass and obesity-associated protein (FTO; IC₅₀ = 142.6 nM in a cell-free assay).¹ It decreases the viability of Mono-Mac-6, NOMO-1, U937, MV4-11, and ML-2 acute myeloid leukemia (AML) cells (IC₅₀s = 58.9-175.9 nM), as well as increases the levels of N⁶-methyladenosine (m⁶A) in Mono-Mac-6 cells at 100 nM. Bisantrene induces apoptosis and cell cycle arrest at the G₀/G₁ phase in NOMO-1 cells. It induces ssDNA breaks and DNA-protein cross-links in L1210 skin lymphocytic leukemia cells when used at a concentration of 10 µg/ml.² Bisantrene (5 mg/kg per day) decreases tumor growth and increases survival time in a patient-derived xenograft (PDX) mouse model of AML.¹ Ex vivo, it induces primary mouse macrophage-mediated cytostasis of P815 mastocytoma cells when co-cultured after administration of a 100 mg/kg dose, an effect that can be inhibited by carrageenan.³

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1. Su, R., Dong, L., Li, Y., et al. Targeting FTO suppresses cancer stem cell maintenance and immune evasion. Cancer Cell 38(1), 79-96 (2020).

2. Bowden, G.T., Garcia, D.E., Peng, Y.-M., et al. Molecular pharmacology of the anthracycline drug 9,10-anthracenedicarboxaldehyde bis[(4,5-dihydro-1 H-imidazol-2-yl)hydrazone] dihydrochloride (Cl 216,942). Cancer Res. 42(7), 2660-2665 (1982).

3. Wang, B.S., Lumanglas, A.L., Ruszala-Mallon, V.M., et al. Activation of tumor-cytostatic macrophages with the antitumor agent 9,10-anthracenedicarboxaldehyde bis[(4,5-dihydro-1H-imidazole-2-yl)hydrazone] dihydrochloride (bisantrene). Cancer Res. 44(6), 2363-2367 (1984).