中文名 | (E)-3PO |
英文名 | 3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one |
别名 | 3PO游离态 (E)-3-吡啶-3-基-1-吡啶-4-基 - 丙烯酮 |
英文别名 | 3 PO 3-PO (E)-3PO inhibitor of glucose metabolism 3PO (inhibitor of glucose metabolism) (E)-3-Pyridin-3-yl-1-pyridin-4-yl-propenone 3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one 2-Propen-1-one, 3-(3-pyridinyl)-1-(4-pyridinyl)-, (2E)- |
CAS | 18550-98-6 |
化学式 | C13H10N2O |
分子量 | 210.23 |
密度 | 1.192±0.06 g/cm3(Predicted) |
沸点 | 387.8±42.0 °C(Predicted) |
溶解度 | 溶于DMSO (高达15 mg/ml) 或乙醇 (高达5 mg/ml) |
酸度系数 | 3.49±0.11(Predicted) |
存储条件 | 2-8°C |
稳定性 | 从提供的购买之日起稳定1年。DMSO或乙醇中的溶液可以在-20 °C下储存长达3个月。 |
外观 | 粉末 |
颜色 | white to beige |
体外研究 | 3PO主要通过与Fru-6-P竞争,抑制PFKFB3,而不抑制纯化的PFK-1活性。在多种人源恶性血液肿瘤和癌细胞系中,3PO可显著地减缓其细胞增殖(IC50=1.4-24 μM)。相较于正常的人类气道上皮细胞,3PO选择性对转染了ras的气道上皮细胞具有抑制生长作用。3PO可引起细胞周期G2-M期阻滞。 |
体内研究 | 向携瘤小鼠腹腔注射0.07 mg的3PO,3PO的给药显著减少了其胞内Fru-2,6-BP的浓度、葡萄糖吸收以及肿瘤的生长。它可抑制乳腺癌、白血病和肺癌细胞的肿瘤生长。向C57Bl/6小鼠静脉注射3PO,检测其在体内药代动力学参数:CL=2312 mL/min/kg, T 1/2=0.3 hr, C max=113 ng/ml, AUC 0-inf=36 ng/hr/ml。在白血病高度相关的小鼠模型中,3PO具有有效抗肿瘤活性。 |
上游原料 | 3-吡啶甲醛 4-乙酰吡啶 |
参考资料 展开查看 | 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. PubMed PMID: 27069123. 2: Biniecka M, Canavan M, McGarry T, Gao W, McCormick J, Cregan S, Gallagher L, Smith T, Phelan JJ, Ryan J, O'Sullivan J, Ng CT, Veale DJ, Fearon U. Dysregulated bioenergetics: a key regulator of joint inflammation. Ann Rheum Dis. 2016 Mar 24. pii: annrheumdis-2015-208476. doi: 10.1136/annrheumdis-2015-208476. [Epub ahead of print] PubMed PMID: 27013493. 3: Saneei A, Pourayoubi M, Crochet A, Fromm KM. The first phosphoramide-mercury(II) complex with a Cl2Hg-OP[N(C)(C)]3 segment. Acta Crystallogr C Struct Chem. 2016 Mar 1;72(Pt 3):230-3. doi: 10.1107/S2053229616002394. Epub 2016 Feb 25. PubMed PMID: 26942433. 4: Nakajima J, Suganami Y, Tsutsumi N, Hirose A, Kondo A, Sunohara D, Kawashima H. Legal Problems Surrounding Medical Care for Neonates Born to International Students: Report of Two Families in Japan. J Immigr Minor Health. 2016 Feb 24. [Epub ahead of print] PubMed PMID: 26911876. 5: Lea MA, Altayyar M, desBordes C. Inhibition of Growth of Bladder Cancer Cells by 3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one in Combination with Other Compounds Affecting Glucose Metabolism. Anticancer Res. 2015 Nov;35(11):5889-99. PubMed PMID: 26504012. 6: Maeda M, Kayano E, Fujiwara T, Nagare H, Akao S. Nitrous oxide emission |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.757 ml | 23.783 ml | 47.567 ml |
5 mM | 0.951 ml | 4.757 ml | 9.513 ml |
10 mM | 0.476 ml | 2.378 ml | 4.757 ml |
5 mM | 0.095 ml | 0.476 ml | 0.951 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!