Drug intelligence / Profile preview

EMAC4001

Development stage
Preclinical
Lead developer
Lithuanian University of Health Sciences
Modality
Small Molecules
01

Overview

EMAC4001 is an experimental small molecule sunitinib analogue belonging to the isatin-dihydropyrazole chemical class. Developed as a potent antineoplastic agent, it has demonstrated significant activity against human pancreatic cancer cell lines, including MIA PaCa-2 and PANC-1, in both normoxic and hypoxic environments. Preclinical studies indicate that EMAC4001 is substantially more potent than sunitinib in inhibiting cell viability and colony formation, suggesting its potential as a targeted therapy for chemotherapy-resistant pancreatic adenocarcinoma. Its mechanism of action likely involves the multi-targeted inhibition of receptor tyrosine kinases, similar to its parent compound sunitinib, but with enhanced potency and selectivity in pancreatic cancer models.

02

Targets

PDGFR (PDGFR family)VEGFR (VEGFR family)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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