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CAS No. : 1450666-80-4
MCE 国际站:UCT943
产品活性:UCT943 是新一代恶性疟原虫 Plasmodium falciparum PI4K 抑制剂。UCT943 抑制 P. vivax PI4K (PvPI4K) 酶,IC50 为 23 nM。
研究领域:PI3K/Akt/mTOR | Anti-infection
作用靶点:PI4K | Parasite
In Vitro: UCT943 maintains high in vitro selectivity (>200-fold) for the parasite PvPI4K versus the human PI4Kβ isozyme (IC50 of PI4Kβ, 5.4 μM), inhibition of which is linked to immunosuppressive effects.
In vitro cytotoxicity of UCT943 is tested against L6 cells, chinese hamster ovarian (CHO), Vero, and HepG2 cells, with 50% cytotoxic concentrations (CC50s) of 12, 17, 113, and 13 μM, respectively.
In Vivo: UCT943 shows excellent in vivo efficacy in the Plasmodium berghei (10 mg/kg and 3 mg/kg; oral administration; daily; 4 days) and P. falciparum NSG (NOD-scid IL-2Rγnull) mouse models (0.01, 0.1, 0.3, 1.1 and 10 mg/kg; oral administration; once per day; 4 days). When dosed at 10 mg/kg per os (p.o.), UCT943 reduces parasitemia by >99.9% in the mouse P. berghei infection model and cures all mice, with >30 mean survival days (MSD). At 3 mg/kg p.o., no complete cure is achieved, and MSD is 10 days, albeit parasitemia is reduced by 99%. The resulting 90% effective dose (ED90) is 1.0 mg/kg p.o. in the P. berghei infection model. The ED90 is 0.25 mg/kg in the P. falciparum-infected NSG mouse model.
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