5MPN|cas:47208-82-2|西域试剂

5MPN,98.0%

产品编号：Bellancom-123981| CAS NO：47208-82-2| 分子式：C₁₅H₁₉N₃O₄| 分子量：305.33

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货号	价格	库存与货期
Bellancom-123981	￥2100.00	杭州北京（现货）
Bellancom-123981	￥3500.00	杭州北京（现货）
Bellancom-123981	￥7000.00	杭州北京（现货）
Bellancom-123981	￥11200.00	杭州北京（现货）

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5MPN

产品介绍

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 (K_i=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。

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 (K_i=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.

体外研究

5MPN (0~30 μM; 24 hours; H460 cells) inhibits the expression of PFKFB4.
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.
5MPN (0 and 10 μM; 6, 12 and 24 hours; H460 cells) induces cells apoptosis.
5MPN (0 and 10 μM; 6, 12 and 24 hours; H460 cells) arrests cell cycle progression.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	H460 cells
Concentration:	0~30 μΜ
Incubation Time:	24 hours
Result:	Inhibited the expression of PFKFB4 .

Cell Proliferation Assay

Cell Line:	H460 NSCLC cells
Concentration:	0~50 μM
Incubation Time:	0~72 hours
Result:	Resulted in a reduction in cell proliferation.

Apoptosis Analysis

Cell Line:	H460 cells
Concentration:	0 and 10 μΜ
Incubation Time:	6, 12 and 24 hours
Result:	Induced cells apoptosis.

Cell Cycle Analysis

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.
5MPN causes a reduction in Ki67-positive cells in the LLC xenografts suggesting that 5MPN may be reducing cell cycle progression in vivo.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 mice
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 mice
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 mice
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (327.51 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2751 mL	16.3757 mL	32.7515 mL
5 mM	0.6550 mL	3.2751 mL	6.5503 mL
10 mM	0.3275 mL	1.6376 mL	3.2751 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： Cremophor EL
Solubility: 20 mg/mL (65.50 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.19 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.19 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.19 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。