Fendiline
Based on 3 publication(s) in Google Scholar
Fendiline, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10).
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- Pureza: 99.41%
- No. CAS: 13042-18-7
- Fòrmula: C23H25N
- Peso molecular:315.45
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Fendiline
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | IC50 |
28.6 μM
Compound: 6
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Antiproliferative activity against human BXPC-3 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human BXPC-3 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| Caco-2 | IC50 |
14.5 μM
Compound: 6
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Antiproliferative activity against human Caco-2 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human Caco-2 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| CHO | EC50 |
1 μM
Compound: Fendiline
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Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay
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[PMID: 23465611] |
| HEC-1-A | IC50 |
9.48 μM
Compound: 6
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Antiproliferative activity against human HEC-1-A cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human HEC-1-A cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| HEC-1B cell line | IC50 |
9.8 μM
Compound: 6
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Antiproliferative activity against human HEC-1B cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human HEC-1B cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| Ishikawa | IC50 |
>30 μM
Compound: 6
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Antiproliferative activity against human Ishikawa cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human Ishikawa cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| MEF | IC50 |
13.1 μM
Compound: 6
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Antiproliferative activity against mouse MEF cells expressing KRAS G12D mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against mouse MEF cells expressing KRAS G12D mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| MEF | IC50 |
17.8 μM
Compound: 6
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Cytotoxicity against mouse MEF cells expressing BRAF V600E mutant and wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Cytotoxicity against mouse MEF cells expressing BRAF V600E mutant and wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| MEF | IC50 |
8.1 μM
Compound: 6
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Antiproliferative activity against mouse MEF cells expressing KRAS G12V mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against mouse MEF cells expressing KRAS G12V mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| MIA PaCa-2 | IC50 |
9.2 μM
Compound: 6
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Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS mutant assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| NCI-H1299 | IC50 |
24.3 μM
Compound: 6
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Antiproliferative activity against human NCI-H1299 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human NCI-H1299 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| NCI-H1975 | IC50 |
>30 μM
Compound: 6
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Antiproliferative activity against human NCI-H1975 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human NCI-H1975 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| NCI-H23 | IC50 |
11.4 μM
Compound: 6
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Antiproliferative activity against human NCI-H23 cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human NCI-H23 cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| NCI-H522 | IC50 |
29.6 μM
Compound: 6
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Antiproliferative activity against human NCI-H522 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human NCI-H522 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| SK-CO-1 | IC50 |
7.8 μM
Compound: 6
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Antiproliferative activity against human SK-CO-1 cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
Antiproliferative activity against human SK-CO-1 cells expressing mutant KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
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[PMID: 33756124] |
| Ventricular myocyte | IC50 |
17 μM
Compound: Fendiline
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Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
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[PMID: 22761000] |
Fendiline (0.3-100 µM) applies extracellularly inhibited the calcium channel current (ICa) in a concentration- and time-dependent manner[1].
Fendiline does not inhibit K-Ras posttranslational processing but significantly reduced nanoclustering of K-Ras and redistributed K-Ras from the plasma membrane to the endoplasmic reticulum (ER), Golgi apparatus, endosomes, and cytosol[2].
Fendiline (17 µM; 48 h) significantly inhibits signaling downstream of constitutively active K-Ras and endogenous K-Ras signaling in cells transformed by oncogenic H-Ras[2].
Fendiline (0-1.25 μM; 72 h) blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras[2].
Fendiline competes for [3H]Yohimbine binding to human platelets α2-adrenergic receptors with a Kd of 2.6 µM[3].
Fendiline (M335) (5-40 μM; 4 h) activates the STING-TBK1-IRF3 axis and induces autophagy (LC3-II upregulation) in a concentration-dependent manner in THP-1 cells[4].
Fendiline (20 μM; 4 h) fails to activate pTBK1, pIRF3, or upregulate IFNB, ISG15, CXCL10, and IL6 in THP-STING KO cells[4].
Fendiline (10-30 μM; 6 h) reduces the viral infection efficiency in a dose - dependent manner in THP-1 cells infected with HSV-1-GFP[4].
Fendiline (20 μM; 6 h) shows stronger antiviral activity against HSV-1-GFP in HeLa-STOE cells overexpressing STING than in STING-deficient HeLa cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDCK cells stably expressing K-RasG12V
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Concentration:2.5 µM, 5 µM, 7.5 µM, 10 µM, 12.5 µM, 15 µM
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Incubation Time:48 h
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Result:Inhibited the ERK and Akt activation with IC50s of 9.49 μM and 6.97 μM, respectively.
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Cell Line:MDCK cells stably expressing K-RasG12V
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Concentration:17 µM
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Incubation Time:48 h
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Result:Significantly reduced pMEK, pERK, and pAkt levels in BHK and MDCK cells expressing constitutively active H-RasG12V.
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Cell Line:THP-1 cells
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Concentration:5 μM, 10 μM, 20 μM, 40 μM
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Incubation Time:2 h, 4 h, 6 h, 8 h
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Result:The protein expression of pTBK1, pIRF3, and LC3-II increased in a concentration-dependent manner, indicating the activation of the STING pathway and autophagy.
Fendiline (5-20 mg/kg; intraperitoneal injection; every 2 days; 20 days) in BALB/c mice inoculated with CT26 or B16F10 tumors inhibits tumor growth in a dose - dependent manner and activates the systemic immune system (increasing CD45+, CD3+, CD8+, and NK+ cells in the spleen)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (female, 6-8 weeks old,) with subcutaneous MC38 tumors[4].
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Dosage:300 μg
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Administration:Intratumoral injection, every 2 days, for 20 days
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Result:The tumor growth inhibition rate (TGI) was 82%.
There was no significant weight loss or organ toxicity.
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Animal Model:BALB/c mice (female, 6-8 weeks old) with subcutaneous CT26 or B16F10 tumors[4].
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Dosage:5 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:Intraperitoneal injection, every 2 days, for 20 days
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Result:There was a dose-dependent tumor growth inhibition.
There was no significant systemic toxicity.
Chemical Information
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No. CAS 13042-18-7
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Appearance Viscous Liquid
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Peso molecular 315.45
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Fòrmula C23H25N
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Color Colorless to light yellow
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SMILES
CC(C1=CC=CC=C1)NCCC(C2=CC=CC=C2)C3=CC=CC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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ACS Nano
2025 Aug 26;19(33):30525-30543. PMID: 40811768 -
J Adv Res
Calcium Influx: An Essential Process by which α-Synuclein Regulates Morphology of Erythrocytes. [Abstract]2024 Aug:62:187-198. PMID: 37714326 -
Mol Pharm
Radionuclide-Aided Improvement of the Therapeutic Efficacy of Novel Antibody-Drug Conjugates against HER2-Expressing Cancers. [Abstract]2025 Jul 7;22(7):3793-3802. PMID: 40448644
Solvente y solubilidad
DMSO : 100 mg/mL (317.01 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (7.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
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.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Tripathi O, et al. Fendiline inhibits L-type calcium channels in guinea-pig ventricular myocytes: a whole-cell patch-clamp study. Br J Pharmacol. 1993 Apr;108(4):865-9. [Content Brief]
[2]. van der Hoeven D, et al. Fendiline inhibits K-Ras plasma membrane localization and blocks K-Ras signal transmission. Mol Cell Biol. 2013 Jan;33(2):237-51. [Content Brief]
[3]. Motulsky HJ, et al. Interaction of verapamil and other calcium channel blockers with alpha 1- and alpha 2-adrenergic receptors. Circ Res. 1983 Feb;52(2):226-31. [Content Brief]
[4]. Zhao M, et al. M335, a novel small-molecule STING agonist activates the immune response and exerts antitumor effects. Eur J Med Chem. 2023 Dec 2;264:116018. [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. 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 | 1 mM | 3.1701 mL | 15.8504 mL | 31.7007 mL | 79.2519 mL |
| 5 mM | 0.6340 mL | 3.1701 mL | 6.3401 mL | 15.8504 mL | |
| 10 mM | 0.3170 mL | 1.5850 mL | 3.1701 mL | 7.9252 mL | |
| 15 mM | 0.2113 mL | 1.0567 mL | 2.1134 mL | 5.2835 mL | |
| 20 mM | 0.1585 mL | 0.7925 mL | 1.5850 mL | 3.9626 mL | |
| 25 mM | 0.1268 mL | 0.6340 mL | 1.2680 mL | 3.1701 mL | |
| 30 mM | 0.1057 mL | 0.5283 mL | 1.0567 mL | 2.6417 mL | |
| 40 mM | 0.0793 mL | 0.3963 mL | 0.7925 mL | 1.9813 mL | |
| 50 mM | 0.0634 mL | 0.3170 mL | 0.6340 mL | 1.5850 mL | |
| 60 mM | 0.0528 mL | 0.2642 mL | 0.5283 mL | 1.3209 mL | |
| 80 mM | 0.0396 mL | 0.1981 mL | 0.3963 mL | 0.9906 mL | |
| 100 mM | 0.0317 mL | 0.1585 mL | 0.3170 mL | 0.7925 mL |
Fendiline Related Classifications
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