Powder: -20°C for 3 years | In solvent: -80°C for 1 year
3PO 是一种 PFKFB3 的小分子抑制剂,IC50值为22.9 μM。它抑制几种人类恶性造血和腺癌细胞系的增殖,IC50在1.4到24 μM 之间。它抑制葡萄糖摄取,并降低 Fru-2,6-BP、乳酸、ATP、NAD+ 和 NADH 的细胞内浓度。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 219 | 现货 | ||
5 mg | ¥ 483 | 现货 | ||
10 mg | ¥ 693 | 现货 | ||
25 mg | ¥ 1,270 | 现货 | ||
50 mg | ¥ 2,080 | 现货 | ||
100 mg | ¥ 3,160 | 现货 | ||
200 mg | ¥ 4,530 | 现货 | ||
500 mg | ¥ 6,870 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 543 | 现货 |
产品描述 | 3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH. |
靶点活性 | PFKFB3:22.9 μM |
体外活性 | 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. Compared with the wild-type PFKFB3+/+transformed cells (IC50, 49 μM), the PFKFB3+/- fibroblasts were more sensitive to compound 3PO treatment (IC50, 26 μM). 3PO Causes G2-M phase arrest, which Is preceded by decreased Fru-2,6-BP and glucose uptake. 3PO slows growth through inhibition of PFK-2 activity, then ectopic expression of the PFKFB3 isozyme may thwart the cytostatic activity of 3PO. [1] 3PO inhibits the glycolytic regulator PFKFB3 in endothelial cells (ECs). 3PO decreases glycolysis in ECs and impairs vessel sprouting. 3PO also suppresses vascular hyperbranching induced by inhibition of Notch or VEGF receptor 1 (VEGFR1) and amplified the antiangiogenic effect of VEGF blockade[2]. |
体内活性 | Compared with vehicle control, compound 3PO treatment significantly reduced Fru-2,6-BP in tumor xenografts (vehicle: 13.1 ± 1.9 pmol/mg, 3PO: 8.5 ± 1.7 pmol/mg). [1] 3PO also impairs (pathological) angiogenesis. |
分子量 | 210.23 |
分子式 | C13H10N2O |
CAS No. | 18550-98-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 113mg/ml(537.51mM)
Ethanol: 11 mg/mL (52.32 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 4.7567 mL | 23.7835 mL | 47.567 mL | 118.9174 mL |
5 mM | 0.9513 mL | 4.7567 mL | 9.5134 mL | 23.7835 mL | |
10 mM | 0.4757 mL | 2.3783 mL | 4.7567 mL | 11.8917 mL | |
20 mM | 0.2378 mL | 1.1892 mL | 2.3783 mL | 5.9459 mL | |
50 mM | 0.0951 mL | 0.4757 mL | 0.9513 mL | 2.3783 mL | |
DMSO | 100 mM | 0.0476 mL | 0.2378 mL | 0.4757 mL | 1.1892 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
3PO 18550-98-6 Autophagy Metabolism Glucokinase isozyme inhibit adenocarcinoma cell human malignant hematopoietic chemotherapeutic agents small-molecule Inhibitor inhibitor