Fendiline hydrochloride

Name: Fendiline hydrochloride
Brand: MedChemExpress
SKU: HY-B0984
Rating: 4.5 (1 reviews)

Cat. No.: HY-B0984 Purity: 99.80%: Data Sheet
SDS

COA
Handling Instructions Technical Support

Solubility

In Vivo Dissolution Calculator

Fendiline hydrochloride, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC₅₀ of 17 µM). Fendiline hydrochloride is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline hydrochloride 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 hydrochloride 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 hydrochloride Chemical Structure

CAS No. : 13636-18-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.2 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: June 3
Solution
10 mM * 1 mL in DMSO	USD 69	In-stock	Estimated Time of Arrival: June 3
Solid
100 mg	USD 63	In-stock	Estimated Time of Arrival: June 3
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Fendiline hydrochloride:

Fendiline Get quote

1 Publications Citing Use of MCE Fendiline hydrochloride

•J Adv Res. 2023 Sep 13;S2090-1232(23)00257-6. [Abstract]

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•Related Screening Libraries:

View All Calcium Channel Isoform Specific Products:

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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:

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K-Ras H-Ras N-Ras Ras

Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

Fendiline (0.3-100 µM) hydrochloride applies extracellularly inhibited the calcium channel current (ICa) in a concentration- and time-dependent manner^[1].
Fendiline hydrochloride 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) hydrochloride 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) hydrochloride blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras^[2].
Fendiline hydrochloride competes for [³H]Yohimbine binding to human platelets α2-adrenergic receptors with a K_d of 2.6 µM^[3].
Fendiline (M335) (5-40 μM; 4 h) hydrochloride 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) hydrochloride fails to activate pTBK1, pIRF3, or upregulate IFNB, ISG15, CXCL10, and IL6 in THP-STING KO cells^[4].
Fendiline (10-30 μM; 6 h) hydrochloride 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) hydrochloride shows stronger antiviral activity against HSV-1-GFP in HeLa-ST^OE 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.

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) hydrochloride 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) hydrochloride 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

351.91

Formula

C₂₃H₂₆ClN

CAS No.

13636-18-5

Appearance

Solid

Color

White to off-white

SMILES

CC(NCCC(C1=CC=CC=C1)C2=CC=CC=C2)C3=CC=CC=C3.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 30 mg/mL (85.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1.82 mg/mL (5.17 mM; ultrasonic and warming and heat to 60°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8416 mL	14.2082 mL	28.4164 mL
5 mM	0.5683 mL	2.8416 mL	5.6833 mL
10 mM	0.2842 mL	1.4208 mL	2.8416 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 (sealed storage, 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.08 mg/mL (5.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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)

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, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Purity & Documentation

Purity: 99.80%

Select Batch:

Data Sheet (294 KB) SDS (393 KB)

COA (248 KB) LCMS (260 KB)

Handling Instructions (2659 KB)

References

[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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.8416 mL	14.2082 mL	28.4164 mL	71.0409 mL
H₂O / DMSO	5 mM	0.5683 mL	2.8416 mL	5.6833 mL	14.2082 mL
DMSO	10 mM	0.2842 mL	1.4208 mL	2.8416 mL	7.1041 mL
	15 mM	0.1894 mL	0.9472 mL	1.8944 mL	4.7361 mL
	20 mM	0.1421 mL	0.7104 mL	1.4208 mL	3.5520 mL
	25 mM	0.1137 mL	0.5683 mL	1.1367 mL	2.8416 mL
	30 mM	0.0947 mL	0.4736 mL	0.9472 mL	2.3680 mL
	40 mM	0.0710 mL	0.3552 mL	0.7104 mL	1.7760 mL
	50 mM	0.0568 mL	0.2842 mL	0.5683 mL	1.4208 mL
	60 mM	0.0474 mL	0.2368 mL	0.4736 mL	1.1840 mL
	80 mM	0.0355 mL	0.1776 mL	0.3552 mL	0.8880 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.