Drug intelligence / Profile preview

Lavendustin A

Development stage
Unknown
Modality
Small Molecules
Administration
In Vitro Research Use; No Approved Clinical Routes Documented
01

Overview

Lavendustin A is a small molecule tyrosine kinase inhibitor originally isolated from *Streptomyces griseolavendus*. It acts as a selective, cell-permeable, reversible, and substrate competitive inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase and p60c-src kinase with little to no inhibition of protein kinase A or C. It inhibits EGFR-associated tyrosine kinase activity with an IC50 around 11 nM and also inhibits tubulin polymerization. Lavendustin A exhibits antitumor activity by blocking these kinases and angiogenesis pathways. Additionally, it has neuroprotective effects by promoting axonal outgrowth in neurons. The compound competitively inhibits ATP binding at the EGFR site but noncompetitively affects peptide substrate binding. It has been used in research to study tyrosine kinase signaling pathways and cancer cell proliferation[1][3][4][5][8][9].

Other names
5-[(2,5-dihydroxyphenyl)methyl-[(2-hydroxyphenyl)methyl]amino]-2-hydroxybenzoic acid5-amino-((N-2,5-dihydroxybenzyl)-N'-2-hydroxybenzyl)aminosalicylic acid
02

Targets

SRC (Proto-oncogene tyrosine-protein kinase Src)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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