Phenformin hydrochloride
Based on 11 publication(s) in Google Scholar
Phenformin (Phenethylbiguanide) hydrochloride is an orally active biguanide hypoglycemic agent. Phenformin hydrochloride inhibits mitochondrial respiratory chain complex I, leading to an increased AMP/ATP ratio, activation of AMPK, and subsequent inhibition of the mTOR pathway, thereby suppressing cell proliferation, inducing apoptosis and autophagy. Phenformin hydrochloride inhibits cancer stem cells (CSCs) and possesses potent antitumor potential.
For research use only. We do not sell to patients.
- Purity: 99.64%
- CAS No.: 834-28-6
- Formula: C10H16ClN5
- Molecular Weight:241.72
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Storage:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Phenformin hydrochloride
More- Nat Commun. 2019 Jul 1;10(1):2901. [Abstract]
- J Nanobiotechnology. 2026 Feb 7;24(1):227. [Abstract]
- Cell Rep Med. 2022 Nov 15;3(11):100802. [Abstract]
- NPJ Precis Oncol. 2026 Mar 6;10(1):156. [Abstract]
- Int J Biol Macromol. 2025 Aug 21;323(Pt 1):147047. [Abstract]
- Mol Syst Biol. 2023 Jul 11;19(7):e11267. [Abstract]
- Life Sci. 2019 Jan 15:217:243-250. [Abstract]
- Cancer Immunol Immunother. 2026 May 22. [Abstract]
- Pharmaceuticals (Basel). 2024 Sep 19;17(9):1234. [Abstract]
- ACS Omega. 2022 Jan 18;7(4):3293-3311. [Abstract]
- Biomed Pharmacother. 2020 Aug:128:110216. [Abstract]
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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WB
All AMPK Isoforms
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Biological Activity
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AMPK |
Phenformin hydrochloride induces G0/G1 cell cycle arrest, reduces the proportion of S phase in a dose-dependent manner, inhibits CDK4 and D glycine, and activates p21 protein in SKOV3, IGROV-1 and Hey ovarian cancer cell lines[1].
Phenformin hydrochloride acts synergistically with SCH772984 (HY-50846) to inhibit proliferation, induce apoptosis, and completely suppress the mTOR signaling pathway in NF1-mutant melanoma cells[1].
Combination treatment with Phenformin hydrochloride and Temozolomide (HY-17364) exerts a synergistic effect on the death of glioblastoma stem cells, thereby enhancing the anti-tumor activity of Phenformin hydrochloride and reducing its required administration concentration[1].
Phenformin (0.5-5 mM; 24-72 h) hydrochloride reduces the viability and promotes apoptosis of SET2 JAK2V617F cells, with corresponding IC50 values of 2 mM, 1.79 mM and 0.79 mM at 24 h, 48 h and 72 h, respectively[2].
Phenformin (2 mM; 12-48 h) hydrochloride inhibits the proliferation of human cholangiocarcinoma cell lines RBE and Huh28 in a time-dependent manner, with significant effects observed at 12, 24 and 48 h[3].
Phenformin (2 mM; 10 days) hydrochloride inhibits the colony-forming ability of human cholangiocarcinoma cell lines RBE and Huh28[3].
Phenformin (2 mM; 24 h) hydrochloride induces apoptosis in human cholangiocarcinoma cell lines RBE and Huh28 after 24 h of treatment[3].
Phenformin (2 mM; 24 h) hydrochloride upregulates the mRNA expression of autophagy-related genes (BECN1, ATG5, ATG7) in human cholangiocarcinoma cell lines RBE and Huh28 after 24 hours of treatment[3].
Phenformin (2 mM; 12-48 h) hydrochloride exerts a significantly stronger inhibitory effect on the viability of LKB1-knockdown RBE and Huh28 human cholangiocarcinoma cell lines than on cells transfected with negative control siRNA at 12, 24, and 48 h[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
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Concentration:2 mM
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Incubation Time:12 h, 24 h, 48 h
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Result:Significantly inhibited proliferation of RBE and Huh28 cells compared to 0 mM controls at 12, 24, and 48 hours, with increasing inhibition over time.
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Cell Line:RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
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Concentration:2 mM
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Incubation Time:24 h
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Result:Significantly increased the apoptosis rate of RBE and Huh28 cells compared to 0 mM controls.
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Cell Line:RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
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Concentration:2 mM
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Incubation Time:24 h
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Result:Significantly elevated the mRNA expression levels of BECN1, ATG5, and ATG7 in RBE and Huh28 cells compared to 0 mM controls.
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Cell Line:LKB1-knockdown RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
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Concentration:2 mM
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Incubation Time:12 h, 24 h, 48 h
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Result:Further reduced the viability of RBE and Huh28 cells treated with phenformin compared to negative control siRNA-transfected cells.
Phenformin (2 mM; intratumoral; every 4 days; 30 days) hydrochloride significantly inhibits RBE tumor volume in a subcutaneous cholangiocarcinoma xenograft mouse model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 Pepboy (female, lethally irradiated, transplanted with bone marrow cells from conditional vavCre knockin Jak2V617F mice)[2]
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Dosage:40 mg/kg
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Administration:i.p.; daily; 45 days
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Result:Increased frequencies of LSK (Lin⁻Sca-1⁺c-Kit⁺), myeloid progenitors (Lin⁻Sca-1⁺c-Kitʰⁱᵍʰ), and multipotent progenitors (MPP: Lin⁻Sca-1⁺c-Kit⁺CD150⁻CD48⁺) in the bone marrow; showed no effects on peripheral blood counts, spleen weight, megakaryocyte count, erythroid precursors frequency, or ex vivo clonogenic capacity.
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Animal Model:BALB/c (nu/nu) (male, 5 weeks old, mean weight 15 g, subcutaneous RBE cell xenograft)[3]
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Dosage:2 mM
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Administration:intratumoral; every 4 days; 30 days
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Result:Exhibited significantly smaller RBE tumor volume compared with the control group after 28 days.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 834-28-6
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Appearance Solid
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Molecular Weight 241.72
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Formula C10H16ClN5
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Color White to off-white
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SMILES
NC(NC(NCCC1=CC=CC=C1)=N)=N.Cl
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Synonyms
Phenethylbiguanide hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Publications (11)
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Journal Impact Factor
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Most Recent
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Nat Commun
An ErbB2/c-Src axis links bioenergetics with PRC2 translation to drive epigenetic reprogramming and mammary tumorigenesis. [Abstract]2019 Jul 1;10(1):2901. PMID: 31263101
Phenformin hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Jul 1;10(1):2901. [Abstract]
Phenformin hydrochloride (Phen) (100 µM; 24 h) markedly reduced Ezh2 and Suz12 protein expression in NIC cells.
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J Nanobiotechnology
Nanozymes subvert pharmacological conventions: insights from counteracting the placental side effects of TiO₂ nanozymes. [Abstract]2026 Feb 7;24(1):227. PMID: 41654860 -
Cell Rep Med
Estrogen-related receptor alpha drives mitochondrial biogenesis and resistance to neoadjuvant chemoradiation in esophageal cancer. [Abstract]2022 Nov 15;3(11):100802. PMID: 36334593
Phenformin hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2022 Nov 15;3(11):100802. [Abstract]
Phenformin hydrochloride (370 µM) strongly potentiated the induction of apoptosis of 298B cells in response to CR.
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NPJ Precis Oncol
Cuproptosis-associated PDHA1 promotes sarcoma progression and immunotherapy responsiveness via the E2F1-PD-L1 axis: a multi-omics and clinical validation study. [Abstract]2026 Mar 6;10(1):156. PMID: 41792370
Phenformin hydrochloride purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2026 Mar 6;10(1):156. [Abstract]
Dose-response curves showing the effect of phenformin (4-10 mM; 48 h) on cell viability in MG63 cells with high (sh-NC) and low PDHA1 expression (sh-PDHA1).
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Int J Biol Macromol
Bacterial cellulose membrane integrating phase-transited lysozyme nanofilm loaded with biguanides for dressing treatment of atopic dermatitis. [Abstract]2025 Aug 21;323(Pt 1):147047. PMID: 40848785 -
Mol Syst Biol
A metabolic map of the DNA damage response identifies PRDX1 in the control of nuclear ROS scavenging and aspartate availability. [Abstract]2023 Jul 11;19(7):e11267. PMID: 37259925
Phenformin hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Syst Biol. 2023 Jul 11;19(7):e11267. [Abstract]
Phenformin hydrochloride (1-20 μM) increased cell survival of U2-OS cells treated with etoposide.
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Life Sci
FTY720 inhibits the activation of pancreatic stellate cells by promoting apoptosis and suppressing autophagy via the AMPK/mTOR pathway. [Abstract]2019 Jan 15:217:243-250. PMID: 30550889 -
Cancer Immunol Immunother
GFI1 enhances MHC-I expression in tumor cells and augments tumor responsiveness to PD-1/PD-L1 inhibitors. [Abstract]2026 May 22. PMID: 42174278 -
Pharmaceuticals (Basel)
2024 Sep 19;17(9):1234. PMID: 39338396
Phenformin hydrochloride purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2024 Sep 19;17(9):1234. [Abstract]
Representative recordings illustrating the NMDA receptors inhibition by Phenformin hydrochloride (Phen) (3-30 μM).
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ACS Omega
Proteomic Changes in the Monolayer and Spheroid Melanoma Cell Models of Acquired Resistance to BRAF and MEK1/2 Inhibitors. [Abstract]2022 Jan 18;7(4):3293-3311. PMID: 35128241 -
Biomed Pharmacother
Saikosaponin A inhibits the activation of pancreatic stellate cells by suppressing autophagy and the NLRP3 inflammasome via the AMPK/mTOR pathway. [Abstract]2020 Aug:128:110216. PMID: 32497863
Solvent & Solubility
H2O : 12.5 mg/mL (51.71 mM; Need ultrasonic)
DMSO : 10 mg/mL (41.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.42 mg/mL (1.74 mM); Clear solution
This protocol yields a clear solution of ≥ 0.42 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.42 mg/mL (1.74 mM); Clear solution
This protocol yields a clear solution of ≥ 0.42 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 2.5 mg/mL (10.34 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. García Rubiño ME, et al. Phenformin as an Anticancer Agent: Challenges and Prospects. Int J Mol Sci. 2019;20(13):3316. Published 2019 Jul 5. [Content Brief]
[2]. Alves-Silva AB, et al. Phenformin increases early hematopoietic progenitors in the Jak2V617F murine model. Invest New Drugs. 2022;40(3):576-585. [Content Brief]
[3]. Hu S, et al. Phenformin inhibits cell proliferation and induces cell apoptosis and autophagy in cholangiocarcinoma. Mol Med Rep. 2018;17(4):6028-6032. [Content Brief]
[4]. Yendapally R, et al. A review of phenformin, metformin, and imeglimin. Drug Dev Res. 2020;81(4):390-401. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 4.1370 mL | 20.6851 mL | 41.3702 mL | 103.4255 mL |
| 5 mM | 0.8274 mL | 4.1370 mL | 8.2740 mL | 20.6851 mL | |
| 10 mM | 0.4137 mL | 2.0685 mL | 4.1370 mL | 10.3425 mL | |
| 15 mM | 0.2758 mL | 1.3790 mL | 2.7580 mL | 6.8950 mL | |
| 20 mM | 0.2069 mL | 1.0343 mL | 2.0685 mL | 5.1713 mL | |
| 25 mM | 0.1655 mL | 0.8274 mL | 1.6548 mL | 4.1370 mL | |
| 30 mM | 0.1379 mL | 0.6895 mL | 1.3790 mL | 3.4475 mL | |
| 40 mM | 0.1034 mL | 0.5171 mL | 1.0343 mL | 2.5856 mL | |
| H2O | 50 mM | 0.0827 mL | 0.4137 mL | 0.8274 mL | 2.0685 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.