Drug intelligence / Profile preview

DCZ3301

Development stage
Preclinical
Modality
Small Molecules
Administration
Intravenous
01

Overview

DCZ3301 is a **novel small molecule aryl-guanidino inhibitor** with preclinical antitumor activity, primarily developed for **hematological malignancies**. It inhibits cell proliferation and induces apoptosis and G2/M cell cycle arrest in multiple cancer cell lines, including **diffuse large B-cell lymphoma (DLBCL)**, **multiple myeloma (MM)**, and **T-cell leukemia/lymphoma**. DCZ3301 acts through targeting several key signaling pathways involved in tumor growth and survival, including **PI3K/AKT**, **ERK1/2**, **JAK2/STAT3**, and it downregulates STAT3 phosphorylation by inhibiting Lyn kinase activation. The agent is selective for tumor cells, inducing apoptosis through mitochondrial dysfunction and the caspase-dependent pathway, with negligible cytotoxicity to normal cells. In preclinical models, DCZ3301 reduces tumor burden and shows synergistic effects with established anti-cancer agents such as bortezomib and panobinostat. It also restores drug sensitivity in resistant cancer cells and is effective in overcoming the tumor-protective effects of the microenvironment, such as IL-6 and VEGF stimulation[1][2][5][6][3][9][7].

Other names
NPS ALX Compound 4a hydrochloride
02

Targets

AKT (RAC-alpha serine/threonine-protein kinase)MAPK3 (Mitogen-activated protein kinase 1)JAK2 (Janus kinase 2)LCK (Proto-oncogene tyrosine-protein kinase Lck)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)STAT3 (Signal Transducer and Activator of Transcription 3)

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