AG-490 (AG490; AG 490; Tyrphostin AG490; Tyrphostin B42; Zinc02557947; Zinc 02557947)是一种JAK2/EGFR抑制剂和酪氨酸磷酸化抑制剂，抑制EGFR靶点(IC50=0.1 μM)，并抑制JAK2活性(IC50=10 μM)。AG 490有效抑制IL-2诱导的T细胞增殖，而且显著抑制酪氨酸磷酸化和DNA-转录因子结合活性，如STAT1, -3, -5a, -5b。另外，通过诱导程序性细胞死亡，AG 490选择性抑制体内外白血病细胞生长，但对正常造血作用无有害影响。AG 490抑制多发性骨髓瘤(MM)细胞增殖，诱导细胞凋亡。AG-490抑制Stat3sm组成型激活，且抑制自发的或IL-2诱导的MF肿瘤细胞生长。
参考文献
[1] Wang LH, et al. JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation ofIL-2-mediated T cell response. J Immunol. 1999 Apr 1;162(7):3897-904.
[2] Davoodi-Semiromi A, et al. The tyrphostin agent AG490 prevents and reverses type 1 diabetes in NOD mice. PLoS One. 2012;7(5): e36079.
[3] Cheppudira BP, et al. Anti-hyperalgesic effects of AG490, a Janus kinase inhibitor, in a rat model of inflammatory pain. Biomed Rep. 2015 Sep;3(5):703-706.
[4] Nielsen M., et al. Constitutive activation of a slowly migrating isoform of Stat3 in mycosis fungoides: tyrphostin AG490 inhibits Stat3 activation and growth of mycosis fungoides tumor cell lines. ProcNatlAcadSci USA. 94: 6764-6769 (1997).
冰袋运输。粉末直接保存于-20℃，有效期3年。建议分装后-20℃干燥保存，避免反复冻融。
