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5MPN

产品编号 T40565 CAS 47208-82-2

5MPN is a novel compound that functions as a highly potent and selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4). This compound demonstrates oral activity and serves as a first-in-class inhibitor. Through competitive inhibition of the F6P binding site, 5MPN effectively hinders the functionality of PFKFB4, with a Ki value of 8.6 μM. Importantly, it exhibits no inhibitory effects on PFK-1 or PFKFB3. By specifically targeting the sugar metabolism of tumors, 5MPN exerts its anti-proliferative effects on various human cancer cell lines.

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5MPN, CAS 47208-82-2

规格	价格/CNY	货期
2 mg	￥ 987	5日内发货
25 mg	￥ 7,170	6-8周
50 mg	￥ 9,320	6-8周

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	5MPN is a novel compound that functions as a highly potent and selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4). This compound demonstrates oral activity and serves as a first-in-class inhibitor. Through competitive inhibition of the F6P binding site, 5MPN effectively hinders the functionality of PFKFB4, with a Ki value of 8.6 μM. Importantly, it exhibits no inhibitory effects on PFK-1 or PFKFB3. By specifically targeting the sugar metabolism of tumors, 5MPN exerts its anti-proliferative effects on various human cancer cell lines.
靶点活性	PFKFB4:8.6 μM (KI)
体外活性	5MPN (0~30 μM; 24 hours; H460 cells) inhibits the expression of PFKFB4[1]. 5MPN (0~50 μM; 0~72 hours; H460 NSCLC cells) first reduces the intracellular concentration of F2,6BP, glycolysis and ATP, which in turn results in a reduction in cell proliferation[1]. 5MPN (0 and 10 μM; 6, 12 and 24 hours; H460 cells) induces cells apoptosis[1]. 5MPN (0 and 10 μM; 6, 12 and 24 hours; H460 cells) arrests cell cycle progression[1]. 5MPN (0.1, 1 or 10 μM) significantly inhibits PFKFB4 activity. 5MPN (H460 cells) leads to a dose-dependent decrease in the intracellular F2,6BP concentration. 5MPN (0~30 μM; over 48 hours; H460, H1299, H441, H522 and A549 cells) makes a dose-dependent reduction in cells growth. 5MPN (0~30 μM; 24 hours; H460 cells) inhibits PFKFB4 expression causing the observed reduction in H460 cell proliferation. 5MPN causes a G1 arrest in LLC cells in vitro similar to H460 cells[1]. Western Blot Analysis[1]Cell Line: H460 cells Concentration: 0~30 μΜ Incubation Time: 24 hours Result: Inhibited the expression of PFKFB4 . Cell Proliferation Assay[1]Cell Line: H460 NSCLC cells Concentration: 0~50 μM Incubation Time: 0~72 hours Result: Resulted in a reduction in cell proliferation. Apoptosis Analysis[1]Cell Line: H460 cells Concentration: 0 and 10 μΜ Incubation Time: 6, 12 and 24 hours Result: Induced cells apoptosis. Cell Cycle Analysis[1]Cell Line: H460 cells Concentration: 0 and 10 μΜ Incubation Time: 6, 12 and 24 hours Result: Arrested cell cycle progression.
体内活性	5MPN (120 mg/kg; p.o.) suppresses the growth of Lewis lung carcinomas (LLC) grown in syngeneic mice and H460 human lung adenocarcinoma xenografts grown in athymic mice without affecting body weight[1]. 5MPN causes a reduction in Ki67-positive cells in the LLC xenografts suggesting that 5MPN may be reducing cell cycle progression in vivo[1]. Animal Model: C57BL/6 mice[1]Dosage: 120 mg/kg Administration: P.o. Result: Suppressed the growth of Lewis lung carcinomas (LLC) grown in syngeneic mice and H460 human lung adenocarcinoma xenografts grown in athymic mice without affecting body weight.

分子量	305.334
分子式	C15H19N3O4
CAS No.	47208-82-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Chesney J, et al. Targeting the sugar metabolism of tumors with a first-in-class 6-phosphofructo-2-kinase (PFKFB4) inhibitor. Oncotarget. 2015;6(20):18001-18011.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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