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PFK-015

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Chemical Structure| 4382-63-2 同义名 : PFK15
CAS号 : 4382-63-2
货号 : A131123
分子式 : C17H12N2O
纯度 : 99%+
分子量 : 260.29
MDL号 : MFCD28099813
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(96.05 mM)，配合低频超声，并水浴加热至45℃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+30% PEG300+water 1.5 mg/mL clear

PO 0.5% CMC-Na 29 mg/mL suspension

生物活性
靶点

  • Autophagy

    PFKFB3, IC50:207 nM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.84mL

0.77mL

0.38mL

19.21mL

3.84mL

1.92mL

38.42mL

7.68mL

3.84mL
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