Cat. No.: HY-16397

Phenformin

(Synonyms: Phenethylbiguanide)

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

Phenformin (Phenethylbiguanide) is an orally active biguanide hypoglycemic agent. Phenformin 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 inhibits cancer stem cells (CSCs) and possesses potent antitumor potential.

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Pureté: 98.02%
CAS No.: 114-86-3
Formule: C₁₀H₁₅N₅
Masse moléculaire:205.26

Stockage:

RT, protect from light.

In solvent -80°C, 1 year , -20°C, 6 months

Phenformin Chemical Structure

CAS No.: 114-86-3

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

Activité biologique

Description

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Cellular Effect

Cell Line	Type	Value	Description	References
UMUC3	IC₅₀	0.25 mM Compound: 12	Antiproliferative activity in human UMUC3 cells assessed as cell growth inhibition Antiproliferative activity in human UMUC3 cells assessed as cell growth inhibition	[PMID: 36205714]

In Vitro

Phenformin 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 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 and Temozolomide (HY-17364) exerts a synergistic effect on the death of glioblastoma stem cells, thereby enhancing the anti-tumor activity of Phenformin and reducing its required administration concentration^[1].
Phenformin (0.5-5 mM; 24-72 h) 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) 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) inhibits the colony-forming ability of human cholangiocarcinoma cell lines RBE and Huh28^[3].
Phenformin (2 mM; 24 h) induces apoptosis in human cholangiocarcinoma cell lines RBE and Huh28 after 24 h of treatment^[3].
Phenformin (2 mM; 24 h) 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) 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.

Apoptosis Analysis^[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.

Real Time qPCR^[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) 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) 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.

Chemical Information

CAS No. 114-86-3
Appearance Solid
Masse moléculaire 205.26
Formule C₁₀H₁₅N₅
Color White to off-white
SMILES

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

Phenethylbiguanide
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

RT, protect from light

In solvent	-80°C	1 year
	-20°C	6 months

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 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 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 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 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 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 : 350 mg/mL (1705.15 mM; Need ultrasonic)

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

4.8719 mL

24.3594 mL

48.7187 mL

5 mM

0.9744 mL

4.8719 mL

9.7437 mL

10 mM

0.4872 mL

2.4359 mL

4.8719 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* 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)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
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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

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O	1 mM	4.8719 mL	24.3593 mL	48.7187 mL	121.7967 mL
	5 mM	0.9744 mL	4.8719 mL	9.7437 mL	24.3593 mL
	10 mM	0.4872 mL	2.4359 mL	4.8719 mL	12.1797 mL
	15 mM	0.3248 mL	1.6240 mL	3.2479 mL	8.1198 mL
	20 mM	0.2436 mL	1.2180 mL	2.4359 mL	6.0898 mL
	25 mM	0.1949 mL	0.9744 mL	1.9487 mL	4.8719 mL
	30 mM	0.1624 mL	0.8120 mL	1.6240 mL	4.0599 mL
	40 mM	0.1218 mL	0.6090 mL	1.2180 mL	3.0449 mL
	50 mM	0.0974 mL	0.4872 mL	0.9744 mL	2.4359 mL
	60 mM	0.0812 mL	0.4060 mL	0.8120 mL	2.0299 mL
	80 mM	0.0609 mL	0.3045 mL	0.6090 mL	1.5225 mL
	100 mM	0.0487 mL	0.2436 mL	0.4872 mL	1.2180 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.

Phenformin

11 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Phenformin

Voir tous les produits spécifiques à Isoform AMPK

Voir tous les produits spécifiques à Isoform mTOR

Activité biologique

Chemical Information

Publications (11)

Solvant et solubilité

Pureté et documentation

Références