丁福明
| 中文名称 | 丁福明 |
|---|---|
| 中文同义词 | 丁福明;丁双胍;化合物 T23837 |
| 英文名称 | 1-butylbiguanide |
| 英文同义词 | Butylbiguanide;Butyldiguanide;Dibetos B;Glybigid;H 224;N1-Butylbiguanide;N-BUTYLBIGUANIDINE;Buformin (base and/or unspecified salts) |
| CAS号 | 692-13-7 |
| 分子式 | C6H15N5 |
| 分子量 | 157.2168 |
| EINECS号 | 2117264 |
| 相关类别 | 医药原料;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 692-13-7.mol |
| 结构式 |  |
丁福明 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) |
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. |