2. Neuronal Signaling Membrane Transporter/Ion Channel GPCR/G Protein MAPK/ERK Pathway Immunology/Inflammation Autophagy
  3. Calcium Channel Ras STING Autophagy
  4. Fendiline

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).

For research use only. We do not sell to patients.

Fendiline Chemical Structure

Fendiline Chemical Structure

CAS No. : 13042-18-7

Size Price Stock Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Liquid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Fendiline:

Fendiline Related Antibodies

Top Publications Citing Use of Products

View All Calcium Channel Isoform Specific Products:

View All Isoforms
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

View All Ras Isoform Specific Products:

View All Isoforms
K-Ras H-Ras N-Ras Ras

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1][2][4].

Cellular Effect
Cell Line Type Value Description References
BXPC-3 IC50
28.6 μM
Compound: 6
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
[PMID: 33756124]
Caco-2 IC50
14.5 μM
Compound: 6
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
[PMID: 33756124]
CHO EC50
1000 nM
Compound: Fendiline
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
[PMID: 23465611]
HEC-1-A IC50
9.48 μM
Compound: 6
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
[PMID: 33756124]
HEC-1B cell line IC50
9.8 μM
Compound: 6
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
[PMID: 33756124]
Ishikawa IC50
> 30 μM
Compound: 6
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
[PMID: 33756124]
MEF IC50
13.1 μM
Compound: 6
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
[PMID: 33756124]
MEF IC50
17.8 μM
Compound: 6
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
[PMID: 33756124]
MEF IC50
8.1 μM
Compound: 6
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
[PMID: 33756124]
MIA PaCa-2 IC50
9.2 μM
Compound: 6
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
[PMID: 33756124]
NCI-H1299 IC50
24.3 μM
Compound: 6
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
[PMID: 33756124]
NCI-H1975 IC50
> 30 μM
Compound: 6
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
[PMID: 33756124]
NCI-H23 IC50
11.4 μM
Compound: 6
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
[PMID: 33756124]
NCI-H522 IC50
29.6 μM
Compound: 6
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
[PMID: 33756124]
SK-CO-1 IC50
7.8 μM
Compound: 6
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
[PMID: 33756124]
Ventricular myocyte IC50
17 μM
Compound: Fendiline
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
[PMID: 22761000]
In Vitro

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.

Fendiline Related Antibodies

Western Blot Analysis[2]

Cell Line: MDCK cells stably expressing K-RasG12V
Concentration: 2.5 µM, 5 µM, 7.5 µM, 10 µM, 12.5 µM, 15 µM
Incubation Time: 48 h
Result: Inhibited the ERK and Akt activation with IC50s of 9.49 μM and 6.97 μM, respectively.

Western Blot Analysis[2]

Cell Line: MDCK cells stably expressing K-RasG12V
Concentration: 17 µM
Incubation Time: 48 h
Result: Significantly reduced pMEK, pERK, and pAkt levels in BHK and MDCK cells expressing constitutively active H-RasG12V.

Western Blot Analysis[4]

Cell Line: THP-1 cells
Concentration: 5 μM, 10 μM, 20 μM, 40 μM
Incubation Time: 2 h, 4 h, 6 h, 8 h
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.
In Vivo

Fendiline (300 μg; intratumoral injection; every 2 days; 20 days) in C57BL/6J mice inoculated with MC38 tumors achieves an 82% tumor growth inhibition rate and increases the numbers of CD8⁺ T cells and NK cells in tumors and spleens[4].
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.

Animal Model: C57BL/6J mice (female, 6-8 weeks old,) with subcutaneous MC38 tumors[4].
Dosage: 300 μg
Administration: Intratumoral injection, every 2 days, for 20 days
Result: The tumor growth inhibition rate (TGI) was 82%.
There was no significant weight loss or organ toxicity.
Animal Model: BALB/c mice (female, 6-8 weeks old) with subcutaneous CT26 or B16F10 tumors[4].
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: Intraperitoneal injection, every 2 days, for 20 days
Result: There was a dose-dependent tumor growth inhibition.
There was no significant systemic toxicity.
Molecular Weight

315.45

Formula

C23H25N
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

CC(C1=CC=CC=C1)NCCC(C2=CC=CC=C2)C3=CC=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1701 mL 15.8504 mL 31.7007 mL
5 mM 0.6340 mL 3.1701 mL 6.3401 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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: ≥ 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).
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
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. 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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Fendiline 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:

Fendiline13042-18-7Calcium ChannelRasSTINGAutophagyCa2+ channelsCa channelsStimulator of Interferon GenesTMEM173MITAERISMPYSantianginal agentL-type calcium channelK-RasMC38CT26 and B16F10Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Fendiline
Cat. No.:
HY-B0984A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.