AG490

Cas No.:	133550-30-8
Chemical Name:	Tyrphostin B42
Synonyms:	N-Benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide;AG-490 (Tyrphostin B42);Tyrphostin AG 490;(E)-N-Benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide;2-Propenamide,2-cyano-3-(3,4-dihydroxyphenyl)-N-(phenylmethyl)-, (2E)-;AG 490;AG-490;(E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide;AG490,AG-490;2-Cyano-3-(3,4-dihydroxyphenyl)-N-(benzyl)-2-propenamide;2-Cyano-3-(3,4-dihydroxyphenyl)-N-(phenylmethyl)-2-propenamide;(2E)-2-Cyano-3-(3,4-dihydroxyphenyl)-N-(phenylmethyl)-2-propenamide;TYRPHOSTIN B42;TYROPHOSTIN AG490;bis-tyrphostin B42;AG 490 (Tyrphostin AG 490);Tyrphostin AG 490 AG 490;Zinc02557947;AG 490, >=98%;AG490;Tyrphostin AG490;alpha-Cyano-(3,4-dihydroxy)-N-benzylcinnamide;(2E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide;SMR001230665;2-C
SMILES:	O([H])C1=C(C([H])=C([H])C(=C1[H])/C(/[H])=C(\C#N)/C(N([H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O)O[H]
Formula:	C17H14N2O3
M.Wt:	294.3047
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	AG-490 is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
In Vivo:	AG490 significantly inhibits the development of type 1 diabetes (T1D) (p = 0.02, p = 0.005; at two different time points). Monotherapy of newly diagnosed diabetic NOD mice with AG490 (1 mg/mouse) markedly results in disease remission in treated animals (n=23) in comparision to the absolute inability (0%; 0/10, p=0.003, Log-rank test) of DMSO and sustained eugluycemia is maintained for several months following drug withdrawal[3]. AG490 (1-10 µg) significantly attenuates ʎ-carrageenan-induced thermal hyperalgesia in a dose-dependent manner. AG490 also reduces mechanical hyperalgesia[4].
In Vitro:	AG490 inhibits the activation of Stat-3 by selectively blocking JAK2. AG490 is used to selectively inhibit JAK/Stat-3 activation. At a dose of 10 μM, Stat-3 phosphorylation is decreased by >95% and cell viability is maintained. AG490 at a dose of 10 μM results in >95% decrease in pStat-3 in EGF-stimulated A431 cells with no effect on Stat-3 mass[1]. AG-490 is a potent inhibitor of the JAK3/STAT, JAK3/AP-1, and JAK3/MAPK pathways and their cellular consequences. AG-490 abolishes IL-2-inducible [3H]thymidine incorporation in a dose-dependent manner, displaying an IC50 of 25 μM. AG-490 potently inhibits IL-2-mediated proliferation in T cells, results distinct from previous studies that showed this agent induced apoptosis in ALL cells while exerting apparently no effects on the growth of mitogen-stimulated normal T cells[2].