Description
AG-490 (Tyrphostin B42) can inhibit EGFR, ErbB2 and JAK2 with IC50 of 0.1 uM, 13.5 uM, and ~10 uM.
Storage
2 years at -20 centigrade
Targets
EGFR, ErbB2, JAK2
Molecular Formula
C17H14N2O3
Chemical Name
(E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide
Solubility
DSMO 59 mg/mL Water
In vitro
AG-490 can potently suppresse IL-2-induced T cell proliferation, a non-JAK2-dependent signal, in a dose-dependent manner, but AG-490 does not alter IL-2R chain expression. AG-490 ablates JAK3 and STAT5a and STAT5b tyrosine phosphorylation in vivo, and it inhibits IL-2-induced STAT1, STAT-3, STAT-5a, and STAT-5b DNA binding. Inhibition of JAK3 by AG-490 also nhibits Shc and ERK1/2 phosphorylation in a dose-dependent manner and IL-2-induced AP-1 DNA binding.
In vivo
In vivo administration of AG-490 causes murine myeloma tumor cell apoptosis but does not inhibit IL-12-mediated macrophage activation and IFN-gamma production by lymphocytes.Combined therapy with AG-490 and IL-12 induces greater antitumor effects than either agent alone in a murine myeloma tumor model.
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