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