Aplidine 是有效的eEF1A2(KD=80 nM) 靶向的抗癌药物。Aplidine具有抗病毒活性，抑制SARS-CoV-2的 IC90为 0.88 nM。Aplidine在多发性骨髓瘤，晚期癌症及 COVID-19 领域有研究的价值。

Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM). Aplidine is a potent anti-cancer agent by targeting eukaryotic translation elongation factor 1 Alpha 2(EEF1A2, Kd = 80 nM).

In hACE2-293T cells, Aplidine exhibits anti–SARS-CoV-2 activity with an IC90 of 0.88 nM. In an established model of human pneumocyte-like cells, Aplidine inhibits SARS-CoV-2 replication with an IC90 of 3.14 nM and a selectivity index of 40.4[1]. Aplidine (20 nM; 1 h) induces a dose-dependent decrease in VEGF secretion in MOLT-4 cells. Aplidine (20 nM; 1 h) does not result in significant inhibition of VEGF-R1 mRNA in normal endothelial cells, which do express VEGFR-1 but do not secrete VEGF[1].

In BALB/c mice expressing human ACE2, Aplidine significantly reduced SARS-CoV-2 infection. 0.3 mg/kg Aplidine group results in a reduction of nearly 2 log units in SARS-CoV-2 viral titers in the lungs, and the 1 mg/kg group leads to a reduction of 1.5 log units[2].

137219-37-5

DMSO:100 mg/mL (90.06 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years