AG-490 is an inhibitor of tyrosine kinases .
As a member of the tyrphostin family, AG-490 is reported to have inhibitory activity against many kinases. It can inhibit the hyperactive JAK2 in B cell precursors of ALL patients, inhibit cytokine-induced activation of JAK2 in eosinophils and suppresses the activation of STAT3 in mycosis fungoides-derived T cells. AG-490 is also found to target JAK3 and its downstream STAT and MAPK signaling pathways. In the IL-2-dependent T cell line, D10, AG-490 suppresses IL-2-induced cell proliferation with IC50 value of 25μM without affecting IL-2R chain expression. It also inhibits IL-2-modulated phosphorylation of STAT5a and STAT5b with IC50 value of 50μM-70μM. Moreover, AG-490 reduces IL-2-induced DNA binding by 78%, 65% and 65% for STAT5a/5b, STAT1 and STAT3, respectively. All these show that AG-490 may provide a beneficial therapeutic by suppressing immunopathological states .
 Wang L H, Kirken R A, Erwin R A, et al. JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response. The Journal of Immunology, 1999, 162(7): 3897-3904.
2. Wang L, Zhang F, et al. "CAFs enhance paclitaxel resistance by inducing EMT through the IL‑6/JAK2/STAT3 pathway." Oncol Rep. 2018 May;39(5):2081-2090. PMID:29565447
|Storage||Store at -20°C|
|Solubility||≥14.7 mg/mL in DMSO, ≥4.73 mg/mL in EtOH with ultrasonic and warming, <2.56 mg/mL in H2O|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Description||AG-490 is a tyrosine kinase inhibitor of JAK2, EGFR, and ErbB2 with IC50 values of ～10 μM, 0.1 μM and 13.5 μM, respectively.|
|IC50||～10 μM||0.1 μM||13.5 μM|
Quality Control & MSDS
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