tcsc0108 AG-490

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Product Description

AG-490 is an tyrosine kinase inhibitor, inhibits EGFR and Stat-3.

IC50 & Target: EGFR and Stat-3[1]

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].

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].

Information

CAS No133550-30-8
FormulaC17H14N2O3
Clinical Informationclinicalinformation
PathwayJAK/STAT Signaling
Protein Tyrosine Kinase/RTK
Autophagy
JAK/STAT Signaling
Stem Cell/Wnt
TargetEGFR
EGFR
Autophagy
STAT
STAT

Specifications

Storage Buffer5% DMSO+40% PEG300+5% Tween80+50% 6.25mg/ml
Purity / Grade>98%
SolubilityDMSO 58.0 mg/mL (197.1 mM)
Ethanol 6.0 mg/mL (20.4 mM)
Water Insoluble
Smilessmiles

Misc Information

Storage InstructionPowder: -20°C for 3 years In Solvent: -80°C 12 months
Alternative NamesTyrphostin AG 490
Observed Molecular Weight294.3
NotesMechanism: AG-490 blocks protein tyrosine kinases by binding to the substrate-binding site.
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