Cat. No.: HY-16397A

Phenformin hydrochloride

(Synonyms: Phenethylbiguanide hydrochloride)

11 Cited Publications

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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.

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Pureté: 99.64%
CAS No.: 834-28-6
Formule: C₁₀H₁₆ClN₅
Masse moléculaire:241.72

Stockage:

4°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Phenformin hydrochloride Chemical Structure

CAS No.: 834-28-6

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (11)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[2]

AMPK

Voir tous les produits spécifiques à Isoform mTOR :

Voir tous les produits spécifiques à Isoform 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 JAK2^V617F 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.

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 Jak2^V617F-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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 834-28-6
Appearance Solid
Masse moléculaire 241.72
Formule C₁₀H₁₆ClN₅
Color White to off-white
SMILES

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

Phenethylbiguanide hydrochloride
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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)

All WBBio/Physico-chemical AssayCell Proliferation/Viability Assay

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Journal Impact Factor

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.
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.
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).
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.
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)

Mechanisms of NMDA Receptor Inhibition by Biguanide Compounds. [Abstract]

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).
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

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.1370 mL

20.6851 mL

41.3702 mL

5 mM

0.8274 mL

4.1370 mL

8.2740 mL

10 mM

0.4137 mL

2.0685 mL

4.1370 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.42 mg/mL (1.74 mM); Clear solution

This protocol yields a clear solution of ≥ 0.42 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.2 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (392 KB)
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- Español - ES (392 KB)
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- Italian - IT (392 KB)
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- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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 Jak2^V617F 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Phenformin hydrochloride

11 Cited Publications

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Phenformin hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Phenformin hydrochloride

Voir tous les produits spécifiques à Isoform mTOR

Voir tous les produits spécifiques à Isoform AMPK

Activité biologique

Chemical Information

Publications (11)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Phenformin hydrochloride Related Classifications