Fendiline (hydrochloride)

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) [1][2][4].

Product Specifications

CAS Number

[13636-18-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Calcium Channel; Ras; STING

Type

Reference compound

Related Pathways

Autophagy; GPCR/G Protein; Immunology/Inflammation; MAPK/ERK Pathway; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Infection; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Fendiline-hydrochloride.html

Purity

99.78

Solubility

DMSO : ≥ 30 mg/mL|H2O : 1.82 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C23H26ClN

Molecular Weight

351.91

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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. |[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.|[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.