HIV-1

Nelfinavir (AG1341) (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice. Animal Model: NOD/SCID mice (bearing U266-luc cells) Dosage: 75 mg/kg Administration: I.p.; 5 days a week for 21 days Result: Decreased MM cell growth in NOD/SCID mice.

Nelfinavir (AG1341) (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells. Nelfinavir inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells. Nelfinavir (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines. Nelfinavir (5 μM; 0-24 hours) decreases the phosphorylation of AKT. Nelfinavir activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system. Cell Proliferation Assay Cell Line: RPMI, LP1, U266, OPM2 and MM1S cells Concentration: 1, 2, 5, 10 μM Incubation Time: 48 hours Result: Inhibited the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines in a dose-dependent manner with an IC 50 of 1-5 μM. Apoptosis Analysis Cell Line: LP1 and U266 cells Concentration: 1-10 μM Incubation Time: 17 hours Result: Induced a dose-dependent increase in the percentage of annexin V + /propidium iodide + cells. Western Blot Analysis Cell Line: U266 cells Concentration: 5 μM Incubation Time: 0-24 hours Result: The level of AKT phosphorylation in U266 cells decreased.

Nelfinavir (AG-1341) 是一种有效的口服生物可利用的 HIV-1 蛋白酶抑制剂 (Ki=2 nM) 用于 HIV 感染。Nelfinavir (AG-1341) 是一种广谱的抗癌剂。