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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Monocarboxylate Transporter (MCT)-AZD3965
AZD3965

Chemical Structure : AZD3965

CAS No.: 1448671-31-5

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AZD3965 (AZD-3965)

货号: PC-43178Not For Human Use, Lab Use Only.

AZD3965 (AZD-3965) is a potent, selective, orally bioavailable monocarboxylate transporter 1 (MCT1) inhibitor with binding IC50 of 1.6 nM, displays 6-fold selectivity over MCT2 and does not inhibit MCT3 or MCT4.

规格 价格 库存 数量
5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3280 In stock
50 mg ￥5280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZD3965 (AZD-3965) is a potent, selective, orally bioavailable monocarboxylate transporter 1 (MCT1) inhibitor with binding IC50 of 1.6 nM, displays 6-fold selectivity over MCT2 and does not inhibit MCT3 or MCT4.
AZD3965 inhibits both lactate efflux and influx into cells and causes an increase in glycolysis and an upregulation of glycolytic enzymes in SCLC and gastric cancer cell lines.
AZD3965 reduces tumor growth and increases intratumor lactate in vivo, enhances radiosensitivity by reducing lactate transport.

物理化学性质&存储条件

分子量 515.506
分子式 C21H24F3N5O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 36 mg/mL
Chemical Name/SMILES

Thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione, 5-[[(4S)-4-hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-

参考文献

1. Polański R, et al. Clin Cancer Res. 2014 Feb 15;20(4):926-937.

2. Bola BM, et al. Mol Cancer Ther. 2014 Dec;13(12):2805-16.

3. Hong CS, et al. Cell Rep. 2016 Feb 23;14(7):1590-1601.

4. Beloueche-Babari M, et al. Cancer Res. 2017 Nov 1;77(21):5913-5924.

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