中文名：AZD3965
英文名：AZD3965
純度：Moligand?，≥98%
貨號：A413743
Cas號：1448671-31-5
存儲溫度：-20°C儲存
運輸條件：超低溫運輸
產(chǎn)品介紹：
Information
AZD3965 AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 ( MCT1 ) inhibitor with a binding affinity of 1.6 nM, 6-fold selective over MCT2. Phase 1.
Targets
MCT1
In vitro
In lymphoma cell lines that preferentially express MCT1, AZD3965 potently inhibits lactate transport and cell growth. AZD3965 inhibits MCT1 activity in cells, and shows higher sensitivity in hypoxia. In H526, HGC27 cells and DMS114 cells, AZD3965 increases intracellular lactate and significantly reduces lactate uptake.
In vivo
In nonobese diabetic scid-γ mice bearing COR-L103 xenografts, AZD3965 (100 mg/kg, p.o.) reduces tumor growth and increased intratumor lactate. In mice bearing H526 tumors, AZD3965 (100 mg/kg, p.o.) causes increased lactate concentration, a reduction in growth and increased radiation sensitivity.
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關(guān)鍵字： 1448671-31-5 ; 39OM5Y4K2F ; HMS3873L03 ; 5-[(4s)-4-hydroxy-4-methyl-1,2-oxazolidine-2-carbonyl]-1-isopropyl-3-methyl-6-{[3-methyl-5-(trifluoromethyl)-2h-pyrazol-4-yl]methyl}thieno[2,3-d]pyrimidine-2,4-dione
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