产品说明书

AZD3965

Print
Chemical Structure| 1448671-31-5 同义名 : -
CAS号 : 1448671-31-5
货号 : A173643
分子式 : C21H24F3N5O5S
纯度 : 99%+
分子量 : 515.506
MDL号 : MFCD28963899
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(203.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 11 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
描述 AZD3965 is engineered to selectively block Monocarboxylate Transporter-1 (MCT1), thus anticipated to affect lactate transport into and out of cells[1]. AZD3965 treatment leads to a 3.7-fold rise in intracellular lactate levels under hypoxic conditions in COR-L103 cells, and increases of 3.7-fold and 3.9-fold in NCI-H1048 cells under normoxic and hypoxic conditions, respectively. In all other scenarios, a less than 1.9-fold increase is observed. These results align with AZD3965's mechanism of blocking lactate transport in cells, reducing cell numbers, and indicate its action through MCT1 inhibition. Furthermore, overexpression of MCT1 in NCI-H1048 cells elevates the EC50 from 0.14 nM to 10.5 nM, supporting the action of AZD3965 via MCT1 inhibition[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.70mL

1.94mL

0.97mL

19.40mL

3.88mL

1.94mL
参考文献

[1]Bola BM, et al. Inhibition of monocarboxylate transporter-1 (MCT1) by AZD3965 enhances radiosensitivity by reducing lactate transport. Mol Cancer Ther. 2014 Dec;13(12):2805-16.

[2]Polanski R, et al. Activity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer. Clin Cancer Res. 2014 Feb 15;20(4):926-37.