製品番号: HY-B0984A

Fendiline

3 Cited Publications

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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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純度: 99.41%
CAS 番号: 13042-18-7
分子式: C₂₃H₂₅N
分子量:315.45

保管条件:

Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Fendiline 構造式

CAS 番号: 13042-18-7

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生物活性
- 製品説明
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (3)
溶剤 & 溶解度
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- 体内
純度とドキュメンテーション
参考文献
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関連分類
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製品説明

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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	1 μM 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]

体外実験

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 K_d 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-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.

体内実験

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.

化学情報

CAS 番号 13042-18-7
性状 Viscous liquid
分子量 315.45
分子式 C₂₃H₂₅N
Color Colorless to light yellow
SMILES

CC(C1=CC=CC=C1)NCCC(C2=CC=CC=C2)C3=CC=CC=C3
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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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ACS Nano

An Activated Gasdermin Mimicking Polymer for Antitumor Immunity. [Abstract]

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

溶剤 & 溶解度

体外:

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)

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

3.1701 mL

15.8504 mL

31.7007 mL

5 mM

0.6340 mL

3.1701 mL

6.3401 mL

10 mM

0.3170 mL

1.5850 mL

3.1701 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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体内:

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: ≥ 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.

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

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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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[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]

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, 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

Keywords

Fendiline

3 Cited Publications

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Fendiline

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MedChemExpress（MCE）の使用を引用している文献 Fendiline

Calcium Channel アイソフォーム固有の製品をすべて表示

Ras アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (3)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Fendiline 関連分類

HY-B0984A 関連分類