Drug intelligence / Profile preview

MELK-In-7

Development stage
Preclinical
Lead developer
University of Texas at Austin
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

MELK-In-7 (also known as MELK-IN-17 or MELK-IN-1) is a selective, small-molecule inhibitor of maternal embryonic leucine zipper kinase (MELK), developed through a collaboration between the University of Texas at Austin and MD Anderson Cancer Center. MELK is a serine/threonine kinase that is overexpressed in various aggressive malignancies, including triple-negative breast cancer (TNBC) and glioblastoma multiforme, where it plays a critical role in promoting cancer stem-like cell (CSC) maintenance, epithelial-to-mesenchymal transition (EMT), and tumor metastasis. By targeting MELK, MELK-In-7 suppresses cell proliferation, migration, invasion, and mammosphere formation in TNBC cells, and has demonstrated dose-dependent tumor growth inhibition in preclinical mouse models.

Other names
MELK inhibitor 17Methyl (Z)-3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-5-carboxylateNintedanib Impurity Linhibitor 17inhibitor17inhibitor-17
02

Targets

CAMK2D (Calcium/calmodulin-dependent protein kinase II delta)MKNK2 (MAP kinase-interacting serine/threonine-protein kinase 2)MELK (Maternal embryonic leucine zipper kinase)MLCK (Myosin light chain kinase)CAMK2G (Calcium/calmodulin-dependent protein kinase II gamma chain)FLT3 (Fms related receptor tyrosine kinase 3)

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