Drug intelligence / Profile preview

SKLB-329

Development stage
Preclinical
Lead developer
Sichuan University
Modality
Small Molecules
Administration
Oral
01

Overview

SKLB-329 is a novel, orally administered multikinase inhibitor developed for the treatment of hepatocellular carcinoma. It inhibits angiogenesis-related kinases including VEGFR1, VEGFR2, VEGFR3, FGFR2, and the tyrosine-protein kinase Src. SKLB-329 acts by inhibiting endothelial cell growth, migration, invasion, and tube formation, demonstrating potent anti-angiogenic activity and inhibiting tumor cell proliferation through down-regulation of Src-mediated FAK and Stat3 signaling pathways. It has shown significant anti-tumor activity in preclinical models, with favorable pharmacokinetic properties and higher potency than sorafenib in some assays[1][2][3][5][9].

02

Targets

RAF1 (c-Raf-1 (Y340D/Y341D))VEGFR2 (Vascular endothelial growth factor receptor 2)SRC (Proto-oncogene tyrosine-protein kinase Src)

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