5MPN

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

5MPN 

5MPN 是一种一流、具有口服活性和选择性的 6-磷酸果糖-2激酶/果糖-2,6-二磷酸酶4 (PFKFB4)抑制剂。5MPN 是 F6P 结合位点的竞争性抑制剂 (Ki=8.6 μM)。5MPN 不抑制 PFK-1 或 PFKFB3。5MPN 靶向肿瘤的糖代谢,可以抑制多种人类癌细胞系的增殖。

5MPN

5MPN Chemical Structure

CAS No. : 47208-82-2

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生物活性

5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines[1].

IC50 & Target

KI: 8.6 μM (PFKFB4)[1]

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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

305.33

Formula

C15H19N3O4

CAS 号

47208-82-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

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