Drug intelligence / Profile preview

compound 402433

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

Compound 402433 is a potent small-molecule antagonist of **Multiple C2 and transmembrane domain-containing protein 1 (MCTP1)**. Identified through structure-based virtual screening, it is designed to target the MCTP1/FYN/MEF2C signaling axis, which is a critical driver of therapy-induced neuroendocrine differentiation (NED) in prostate cancer. By antagonizing MCTP1, a calcium-sensing protein, the compound disrupts the downstream activation of the Src-family kinase FYN and the transcription factor MEF2C. In preclinical models of neuroendocrine prostate cancer (NEPC), compound 402433 has demonstrated the ability to significantly reduce tumor burden, decrease alkaline phosphatase (ALPL) enzymatic activity, and attenuate the expression of neuroendocrine markers, suggesting its potential as a therapeutic strategy for treatment-refractory, aggressive prostate cancer phenotypes.

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