产品描述:
Bisantrene is an inhibitor of fat mass and obesity-associated protein (FTO; IC50 = 142.6 nM in a cell-free assay).{51821} 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.{51822} Bisantrene (5 mg/kg per day) decreases tumor growth and increases survival time in a patient-derived xenograft (PDX) mouse model of AML.{51821} 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.{51823}