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) [1][2][4].

Product Specifications

CAS Number

[13042-18-7]

UNSPSC

12352005

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-anti-virus

Field of Research

Cancer; Infection; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/fendiline.html

Purity

99.41

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C23H25N

Molecular Weight

315.45

References & Citations

[1]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.|[2]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.|[3]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.|[4]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.