2. Apoptosis Metabolic Enzyme/Protease Autophagy PI3K/Akt/mTOR Epigenetics
  3. Autophagy mTOR Apoptosis Mitochondrial Metabolism AMPK
  4. Phenformin hydrochloride

Phenformin hydrochloride  (Synonyms: Phenethylbiguanide hydrochloride)

Cat. No.: HY-16397A Purity: 99.64%
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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.

CAS No. : 834-28-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
500 mg In-stock
1 g In-stock
5 g In-stock
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50 g   Get quote  

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Phenformin hydrochloride:

Phenformin hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Phenformin hydrochloride purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2026 Mar 6;10(1):156.

    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).

    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).

    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.

    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.

    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.

    View All mTOR Isoform Specific Products:

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    mTOR mTORC1 mTORC2

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    NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2][3][4].

    IC50 & Target[2]

    AMPK

     

    In Vitro

    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.

    Phenformin hydrochloride Related Antibodies

    Cell Viability Assay[3]

    Cell Line: RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
    Concentration: 2 mM
    Incubation Time: 12 h, 24 h, 48 h
    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.

    Cell Cytotoxicity Assay[3]

    Cell Line: RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
    Concentration: 2 mM
    Incubation Time: 24 h
    Result: Significantly increased the apoptosis rate of RBE and Huh28 cells compared to 0 mM controls.

    RT-PCR[3]

    Cell Line: RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
    Concentration: 2 mM
    Incubation Time: 24 h
    Result: Significantly elevated the mRNA expression levels of BECN1, ATG5, and ATG7 in RBE and Huh28 cells compared to 0 mM controls.

    Cell Viability Assay[3]

    Cell Line: LKB1-knockdown RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
    Concentration: 2 mM
    Incubation Time: 12 h, 24 h, 48 h
    Result: Further reduced the viability of RBE and Huh28 cells treated with phenformin compared to negative control siRNA-transfected cells.
    In Vivo

    Phenformin (40 mg/kg; i.p.; daily; 45 days) hydrochloride increases the percentages of LSK, myeloid progenitor, and multipotent progenitor populations but does not reduce disease burden in Jak2V617F-knockin MPN mice[2].
    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.

    Animal Model: C57BL/6 Pepboy (female, lethally irradiated, transplanted with bone marrow cells from conditional vavCre knockin Jak2V617F mice)[2]
    Dosage: 40 mg/kg
    Administration: i.p.; daily; 45 days
    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.
    Animal Model: BALB/c (nu/nu) (male, 5 weeks old, mean weight 15 g, subcutaneous RBE cell xenograft)[3]
    Dosage: 2 mM
    Administration: intratumoral; every 4 days; 30 days
    Result: Exhibited significantly smaller RBE tumor volume compared with the control group after 28 days.
    Clinical Trial
    Molecular Weight

    241.72

    Formula

    C10H16ClN5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC(NC(NCCC1=CC=CC=C1)=N)=N.Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    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)

    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.1370 mL 20.6851 mL 41.3702 mL
    5 mM 0.8274 mL 4.1370 mL 8.2740 mL
    View the 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.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.

    • Protocol 1

      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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: 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)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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

    Purity: 99.64%

    SDS (392 KB)

    COA (244 KB) Elemental Analysis Report (103 KB)

    Handling Instructions (2659 KB)
    References

    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.

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    Phenformin hydrochloride Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Phenformin834-28-6PhenethylbiguanideAutophagymTORApoptosisMitochondrial MetabolismAMPKMammalian target of RapamycinAMP-activated protein kinaseInhibitorinhibitorinhibit

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