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Buformin hydrochloride (NSC-528218; NSC528218; 1-butylbiguanide) is an orally available AMPK activator used as an antidiabetic drug belonging to the biguanide class. It is chemically/structurally related to metformin and phenformin. Buformin acts by decreasing hepatic gluconeogenesis and lowering blood glucose production in vivo. Buformin was marketed by Grünenthal (a German pharmaceutical company) as Silubin. Buformin delays absorption of glucose from the gastrointestinal tract, increases insulin sensitivity and glucose uptake into cells, and inhibits synthesis of glucose by the liver. Buformin and the other biguanides are not hypoglycemic, but rather antihyperglycemic agents. They do not produce hypoglycemia; instead, they reduce basal and postprandial hyperglycemia in diabetics.[5] Biguanides may antagonize the action of glucagon, thus reducing fasting glucose levels.
| ln Vitro |
The concentration-dependent inhibition of SKBR3 and BT474 cell growth is observed with buformin hydrochloride (0-10 mM; 5 days); IC50s for erbB-2-overexpressing SKBR3 and BT474 cells are 246.7 μM and 98.6 μM, respectively [1]. Buformin hydrochloride (0–3 mM; 48 hours) reduces the percentage of cells in the S phase and raises the proportion of cells in the G0/G1 phase, particularly in SKBR3 cells [1]. As well as inhibiting Akt activation/phosphorylation in SKBR3 and BT474 cells, buformin hydrochloride (0-3 mM; 24 hours) inhibits RTK activation, including downstream erbB-2 and IGF1R signaling [1].
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| ln Vivo |
In MMTV-erbB-2 transgenic mice, buformin hydrochloride (oral; 7.6 mmol/kg, mixed in diet; 7 days) dramatically lowers tumor volume and weight and inhibits the growth and morphogenesis of the mammary glands [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: ErbB-2-overexpressing SKBR3 and BT474 cells Tested Concentrations: 0 μM, 1 μM, 3 μM, 10 μM, 30 μM, 100 μM, 300 μM, 1, 3, or 10 mM Incubation Duration: 5 days Experimental Results: decreased cell viability in erbB-2-overexpressing breast cells. Cell Cycle Analysis[1] Cell Types: ErbB-2-overexpressing SKBR3 and BT474 cells Tested Concentrations: 0.5 mM; 1 mM; 3 mM Incubation Duration: 48 hrs (hours) Experimental Results: Increased cells arresting in G0/G1 phase. Western Blot Analysis[1] Cell Types: ErbB-2-overexpressing SKBR3 and BT474 cells Tested Concentrations: 0mM, 0.1mM, 0.3mM, 1mM, or 3mM Incubation Duration: 24 hrs (hours) Experimental Results: diminished p-AMPK, p-p706S, p-ERK1/2 expression in a concentration-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Female MMTV-erbB-2 transgenic mice[1]
Doses: 7.6 mmol/kg Route of Administration: Oral administration; 7 days Experimental Results: Inhibited mammary syngeneic tumor growth in MMTV-erbB-2 transgenic mice. |
| References |
[1]. Amanda B Parris, et al. Buformin hydrochloride Inhibits the Stemness of erbB-2-overexpressing Breast Cancer Cells and Premalignant Mammary Tissues of MMTV-erbB-2 Transgenic Mice. J Exp Clin Cancer Res
[2]. Jing Li, et al. Buformin hydrochloride Suppresses Proliferation and Invasion via AMPK/S6 Pathway in Cervical Cancer and Synergizes With Paclitaxel. Cancer Biol Ther. 2018 Jun 3;19(6):507-517. |
| Molecular Formula |
C6H16CLN5
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|---|---|
| Molecular Weight |
193.68
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| Exact Mass |
193.1094
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| CAS # |
1190-53-0
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| Related CAS # |
Buformin;692-13-7
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| SMILES |
N=C(NC(N)=N)NCCCC.[H]Cl
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| InChi Key |
KKLWSPPIRBIEOV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H15N5.ClH/c1-2-3-4-10-6(9)11-5(7)8/h2-4H2,1H3,(H6,7,8,9,10,11)1H
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| Chemical Name |
1-Butylbiguanide monohydrochloride
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| Synonyms |
NSC 528218 Silubin NSC-528218Buformin hydrochloride NSC528218
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~645.39 mM)
H2O : ~100 mg/mL (~516.32 mM) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.1632 mL | 25.8158 mL | 51.6316 mL | |
| 5 mM | 1.0326 mL | 5.1632 mL | 10.3263 mL | |
| 10 mM | 0.5163 mL | 2.5816 mL | 5.1632 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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