丁福明
- CAS号:692-13-7
- 英文名:1-butylbiguanide
- 中文名:丁福明
- CBNumber:CB7913312
- 分子式:C6H15N5
- 分子量:157.2168
- MOL File:692-13-7.mol
- 熔点 :174-176 °C
- 沸点 :271.89°C (rough estimate)
- 密度 :1.0291 (rough estimate)
- 折射率 :1.8070 (estimate)
- 酸度系数(pKa) :12.27±0.10(Predicted)
丁福明性质、用途与生产工艺
- 生物活性 Buformin (1-Butylbiguanide) 是一种有效的 AMPK 活化剂，也是具有口服活性的双胍类降血糖试剂 (antidiabetic agent)。Buformin 降低肝糖异生并降低血糖生成。Buformin 也具有抗癌活性，可以应用于癌症研究，如宫颈癌、乳腺癌等。
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体外研究
Buformin (0-10 mM; 5 days) inhibits SKBR3 and BT474 cells growth as a concentration-dependent manner, exhibits IC 50 values of 246.7 μM and 98.6 μM for erbB-2-overexpressing SKBR3 and BT474 cells, respectively.Buformin (0-3 mM; 48 hours) increases the percentage of cells in G0/G1 phase and reduced the percentage of cells in S phase, especially in the SKBR3 cells.Buformin (0-3 mM; 24 hours) suppresses RTK activation, including erbB-2 and IGF1R signaling downstream, and Akt activation/phosphorylation is inhibited in both SKBR3 and BT474 cells.
Cell Viability Assay
Cell Line: ErbB-2-overexpressing SKBR3 and BT474 cells Concentration: 0 μM, 1 μM, 3 μM, 10 μM, 30 μM, 100 μM, 300 μM, 1, 3, or 10 mM Incubation Time: 5 days Result: Reduced cell viability in erbB-2-overexpressing breast cells. Cell Cycle Analysis
Cell Line: ErbB-2-overexpressing SKBR3 and BT474 cells Concentration: 0.5 mM; 1 mM; 3 mM Incubation Time: 48 hours Result: Increased cells arresting in G0/G1 phase. Western Blot Analysis
Cell Line: ErbB-2-overexpressing SKBR3 and BT474 cells Concentration: 0 mM, 0.1 mM, 0.3 mM, 1 mM, or 3 mM Incubation Time: 24 hours Result: Decreased p-AMPK, p-p706S, p-ERK1/2 expression in a concentration-dependent manner. -
体内研究
Buformin (oral administation; 7.6 mmol/kg of chow; 7 days) exhibits significantly reduced tumor volumes and weights, and hinders mammary morphogenesis and proliferation in MMTV-erbB-2 transgenic mice
Animal Model: Female MMTV-erbB-2 transgenic mice Dosage: 7.6 mmol/kg Administration: Oral administation; 7 days Result: Inhibited mammary syngeneic tumor growth in MMTV-erbB-2 transgenic mice. - 类别 有毒物品
- 毒性分级 高毒
- 急性毒性 口服-小鼠 LD50: 300 毫克/公斤; 腹腔-小鼠 LD50: 140 毫克/公斤
- 可燃性危险特性 热分解排出有毒氮氧化物烟雾
- 储运特性 仓库通风低温干燥; 与食品原料分开存放
- 灭火剂 水,干粉, 二氧化碳, 泡沫
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