丁福明
中文名称:
丁福明
中文同义词:
丁福明;丁双胍
英文名称:
1-butylbiguanide
英文同义词:
N-BUTYLBIGUANIDINE;Buformin;Buformin (base and/or unspecified salts);Buformine;Butformin;Butylbiguanide;Butyldiguanide;DBV
CAS号:
692-13-7
分子式:
C6H15N5
分子量:
157.22
EINECS号:
211-726-4
相关类别:
医药原料;Intermediates Fine Chemicals;Pharmaceuticals
Mol文件:
692-13-7.mol
沸点
271.89°C (rough estimate)
密度
1.0291 (rough estimate)
折射率
1.8070 (estimate)
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。
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.
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 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.
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.
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
