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PFK-015
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PFK-015图片
CAS NO:4382-63-2
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
PFK-015 是 3PO 的衍生物,是一种特异性 PFKFB3 抑制剂。
Cas No.4382-63-2
Canonical SMILESO=C(C1=CC=NC=C1)/C([H])=C([H])/C2=NC3=CC=CC=C3C=C2
分子式C17H12N2O
分子量260.29
溶解度≥ 13mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PFK-015 is a potent and selective inhibitor of PFKFB3 with IC50 value of 207 nM [1].

6-phosphofructo-2-kinase (PFKFB3) is an enzyme that is encoded by the PFKFB3 gene in humans. PFKFB3 is a direct transcriptional target of HIF-α and is activated by oncogenic AKT and Ras and stabilized by the loss of the tumor suppressor PTEN via suppressive effects on APC/Cdh1-mediated ubiquitination [1].

PFK-015 is a potent and selective PFKFB3 inhibitor. In H522 lung adenocarcinoma and Jurkat cell lines, PFK15 exhibited cytotoxic effects with IC50 values of 2.42 and 0.72 μM in Jurkat and H522, respectively. Also, PFK15 reduced glucose uptake, intracellular ATP and F26BP, the substrate of PFKFB3. In Jurkat T cell leukemia cells, PFK15 (3 μM) increased the number of cells undergoing early apoptosis. PFK15 (3 and 20 μM) increased the number of cells undergoing late apoptosis in a dose dependent way [1].

In Lewis lung carcinoma (LLC)-bearing mice, PFK15 inhibited LLC cells metastasized from the subcutaneous to the lungs. PFK15 decreased tumor-associated F26BP and significantly increased the number of cells that were positive for cleaved caspase 3. Also, PFK15 reduced fluoro-D-glucose (18F-FDG) uptake by 50%. PFK15 inhibited the growth of colon and pancreatic adenocarcinomas [1].

Reference:
[1].  Clem BF, O'Neal J, Tapolsky G, et al. Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer. Mol Cancer Ther, 2013, 12(8): 1461-1470.