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丁福明
产品纠错
CAS号:692-13-7 | 英文名称:1-butylbiguanide
分子式 C6H15N5
分子量 157
EINECS号 2117264
MDL MFCD00242653
Smiles C(=N)(NCCCC)NC(=N)N
InChIKey XSEUMFJMFFMCIU-UHFFFAOYSA-N
乙二醇化学百科
基本信息
中文名称 丁福明
英文名称 1-butylbiguanide
CAS号 692-13-7
分子式 C6H15N5
分子量 157.2168
EINECS号 2117264
物化性质
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)
安全信息
生产及用途
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。

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.

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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