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抑制剂描述:

产品名称:AZD3965

产品别名:见爱必信官网

英文别名:AZD3965

靶点:MCT

CAS:1448671-31-5

纯度:≥98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (<b>MCT1</b>) inhibitor with a binding affinity of 1.6 nM, 6-fold selective over MCT2. Phase 1.

溶解性:DMSO : 100 mg/mL (193.98 mM; Need ultrasonic)

体外研究:

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.

体内研究: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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