Drug intelligence / Profile preview

ag490

Development stage
Preclinical
Modality
Small Molecules
Administration
In Vitro, Intraplantar (in Animal Models)
01

Overview

**AG490** is a synthetic small molecule that acts as a potent and selective inhibitor of Janus kinase 2 (JAK2) and is also known to inhibit epidermal growth factor receptor (EGFR) tyrosine kinase autophosphorylation. AG490 disrupts the JAK2/STAT pathway, inhibiting cell growth, inducing apoptosis, and blocking DNA synthesis in certain cancer cell lines such as acute lymphoblastic leukemia (ALL). It is widely used as a research tool to study JAK/STAT signaling mechanisms, inflammation, pain models, and cytokine signaling. AG490 is cell-permeable and shows selectivity over other tyrosine kinases, with little effect on normal hematopoiesis. Its effects on blocking IL-6 cytokine signaling and reducing inflammatory markers have been demonstrated in various models. The compound is not approved for human use and is restricted to in vitro or laboratory research applications[1][2][3][4][5][6][7][8][9][10].

Brand names
AG490AG-490AG 490
Other names
Tyrphostin AG490Tyrphostin B42α-Cyano-(3,4-dihydroxy)-N-benzylcinnamide(E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamideN-Benzyl-3,4-dihydroxybenzylidenecyanoacetamide
02

Targets

GUCY2C (Guanylate cyclase C receptor)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)STAT5A (STAT5)JAK2 (Janus kinase 2)ERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)JAK3 (Janus kinase 3)

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