Drug intelligence / Profile preview

compound 15d

Development stage
Preclinical
Lead developer
National Research Centre
Modality
Small Molecules
Administration
Subcutaneous, Intranasal
01

Overview

Compound 15d is a synthetic small molecule quinazoline-quinoxaline hybrid that acts as a multi-target tyrosine kinase inhibitor, with primary activity against Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2). It was designed based on the pharmacophoric features of known VEGFR-2 inhibitors like sorafenib. In preclinical evaluations, 15d demonstrated potent inhibition of VEGFR-2 (IC50 = 60.00 nM) and showed cross-reactivity with Human Epidermal Growth Factor Receptor 2 (HER2; IC50 = 253 nM) and Fibroblast Growth Factor Receptor (FGFR; IC50 = 381 nM). The compound exhibits significant antitumor activity against hepatocellular carcinoma (HepG2), prostate cancer (PC3), and breast cancer (MCF-7) cell lines. Its mechanism of action involves the induction of apoptosis, characterized by the significant upregulation of pro-apoptotic markers including Caspase-3, BAX, and P53.

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)FGFR (Fibroblast growth factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)

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