| 中文名称 | 盐酸丁双胍 |
| 英文名称 | BuforMin Hydrochloride |
| CAS号 | 1190-53-0 |
| 分子式 | C6H16ClN5 |
| 分子量 | 193.68 |
| EINECS号 | 214-723-6 |
| 熔点 | 177-179?C |
| 溶解度 | DMSO（少许）、甲醇（少许）、水（少许） |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
| 稳定性 | 吸湿性 |
| 危险类别码 | 22-43-36 |
| 安全说明 | 36/39-46 |
| 海关编码 | 29212900 |
| 毒性 | LD50 i.p. in mice: 380 mg/kg (Rikimaru) |
Buformin hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (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. |
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