AZD3965
| CAS号 | 1448671-31-5 | 货号 | BCP17734 |
| 中文名 | AZD3965 | ||
| 英文名 | AZD3965 | ||
| 中文别名 | |||
| 英文别名 | AZD-3965;AZD 3965; | ||
| 分子式 | C21H24F3N5O5S | 分子量 | 515.51 |
| 生物活性 | AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM. In vivo, AZD3965 is well tolerated and induces a dose and time dependent accumulation of lactate in the tumours, suppresses tumour growth and in the Raji model potentiates the effects of Rituxan, doxorubicin and bendamustine. The selective inhibition of lactate transport by the MCT1 inhibitor AZD3965 offers an novel mechanism for targeting the metabolic phenotype in tumours that preferentially express MCT1. | ||
| 信号通路 | Ion Channel/Membrane Transporter | ||
| 靶 点 | MCT | ||
结构式
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