DMUP is a potent CD47-SIRPα axis inhibitor. DMUP induces apoptosis and increases the macrophage phagocytosis in A549 cells. DMUP decreases the expression of CD47 and SIRPα protein. DMUP shows antitumor activity [1].
In Vivo, DMUP (10 mg/kg, i.v., every other day for 17 day) shows antitumor activity[1]. DMUP (5, 10, 20, 40 mg/kg, i.v.,every two days for 18 days) shows no toxicity in mice[1].
In Vitro, DMUP (72 h) shows antiproliferative activity with IC50s of 0.92, 3.58, 6.29, 1.54 μM for A549, A549/DDP, PANC-1, HepG2 cells, respectively[1]. DMUP (5 μM, 24 h) arrests the cell cycle in S phase in A549 cells[1]. DMUP (5 μM, 48 h) induces apoptosis in A549 cells[1]. DMUP (5 μM, 24 h) decreases the expression of CD47 and SIRPα protein[1]. DMUP (5 μM, 4 h) increases the macrophage phagocytosis in A549-GFP cells[1].
References:
[1]. Tan Y, et al. Platinum(IV) complexes as inhibitors of CD47-SIRPα axis for chemoimmunotherapy of cancer. Eur J Med Chem. 2022; 229:114047.
In Vivo, DMUP (10 mg/kg, i.v., every other day for 17 day) shows antitumor activity[1]. DMUP (5, 10, 20, 40 mg/kg, i.v.,every two days for 18 days) shows no toxicity in mice[1].
In Vitro, DMUP (72 h) shows antiproliferative activity with IC50s of 0.92, 3.58, 6.29, 1.54 μM for A549, A549/DDP, PANC-1, HepG2 cells, respectively[1]. DMUP (5 μM, 24 h) arrests the cell cycle in S phase in A549 cells[1]. DMUP (5 μM, 48 h) induces apoptosis in A549 cells[1]. DMUP (5 μM, 24 h) decreases the expression of CD47 and SIRPα protein[1]. DMUP (5 μM, 4 h) increases the macrophage phagocytosis in A549-GFP cells[1].
References:
[1]. Tan Y, et al. Platinum(IV) complexes as inhibitors of CD47-SIRPα axis for chemoimmunotherapy of cancer. Eur J Med Chem. 2022; 229:114047.