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CAS No.: 4382-63-2

PFK-015 Catalog No. CSN13931

Synonyms: PFK15

PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.

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实验方案

技术信息

生物活性

描述PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM. PFK15 can produce effective growth inhibition in a series of cancer cells. PFK15 also reduced F26BP (fructose 2,6-bisphosphate), glucose uptake, and intracellular ATP levels in Jurkat T-cell leukemia cells and H522 lung adenocarcinoma cells. PFK15 causes a rapid induction of apoptosis in transformed cells, has adequate pharmacokinetic properties, suppresses the glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in three human xenograft models of cancer in athymic mice that are comparable to U.S. Food and Drug Administration-approved chemotherapeutic agents^[3]. The antitumor drug PFK-158 and its analogs PFK-015 and 3PO can exert synergistic effects with colistin against colistin-resistant Enterobacteriaceae, including mcr-1-positive or high-level-colistin-resistant (HLCR) isolates, as shown by a checkerboard assay^[4].
参考文献

[1] Lea MA, Guzman Y, Desbordes C. Inhibition of Growth by Combined Treatment with Inhibitors of Lactate Dehydrogenase and either Phenformin or Inhibitors of 6-Phosphofructo-2-kinase/Fructose-2,6-bisphosphatase 3. Anticancer Res. 2016 Apr;36(4):1479-88.
[2] Clem BF, O'Neal J, et al. Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer. Mol Cancer Ther. 2013 Aug;12(8):1461-70.
[3] Clem BF, O'Neal J, Tapolsky G, Clem AL, Imbert-Fernandez Y, Kerr DA 2nd, Klarer AC, Redman R, Miller DM, Trent JO, Telang S, Chesney J. Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer. Mol Cancer Ther. 2013 Aug;12(8):1461-70
[4] Zhang Y, Wang X, Li X, Dong L, Hu X, Nie T, Lu Y, Lu X, Pang J, Li G, Yang X, Li C, You X. Synergistic Effect of Colistin Combined with PFK-158 against Colistin-Resistant Enterobacteriaceae. Antimicrob Agents Chemother. 2019 Jun 24;63(7):e00271-19

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8419 mL
- 19.2093 mL
- 38.4187 mL
- 5 mM
- 0.7684 mL
- 3.8419 mL
- 7.6837 mL
- 10 mM
- 0.3842 mL
- 1.9209 mL
- 3.8419 mL

技术信息

CAS号

4382-63-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H12N2O

运输

蓝冰

分子量

260.29

别名

PFK15

溶解度

DMSO	75.0 mg/mL (288.1 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	1.5 mg/mL	clear
PO	0.5% CMC-Na	29 mg/mL	suspension

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