• Specific and potent JAK-2 protein tyrosine kinase inhibitor. Also inhibits EGF receptor autophosphorylation, with an IC50 of 100 nM. Inhibits DNA synthesis and cell growth; induces apoptosis. Levitzki, A. "Tyrphostins--potential antiproliferative agents and novel molecular tools." Biochem. Pharmacol. 40: 913-918 (1990). Gazit, A., et al. "Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases." J. Med. Chem. 34: 1896-1907 (1991).
• Inhibits the growth of leukemic cells in vitro and in vivo. Blocks STAT3 constitutive activation and inhibits both interleukin 2(IL2)-induced and spontaneous growth of Mycosis fungoides (MF), a cutaneous T cell lymphoma. Growth of human ovarian and breast cancer cell lines was shown to be significantly suppressed by AG 490 via JAK/STAT3 pathway inhibition. Meydan, N., et al. "Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor." Nature 379: 645-648 (1996). 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." Proc Natl Acad Sci USA. 94: 6764-6769 (1997). Eriksen, K.W., et al. "Constitutive STAT3-activation in Sezary syndrome: tyrphostin AG490 inhibits STAT3-activation, interleukin-2 receptor expression and growth of leukemic Sezary cells." Leukemia 15: 787-793 (2001). Burke W.M., et al. "Inhibition of constitutively active Stat3 suppresses growth of human ovarian and breast cancer cells." Oncogene 20: 7925-7934 (2001). Levitzki, A. "Tyrosine kinases as targets for cancer therapy." Eur J Cancer 38 Suppl 5: S11-S18 (2002). Burdelya L., et al. "Combination therapy with AG-490 and interleukin 12 achieves greater antitumor effects than either agent alone." Mol Cancer Ther 11: 893-899 (2002).
• AG 490 is a JAK3/STAT, JAK3/AP-1, and JAK3/MAPK signaling pathway inhibitor and also blocks JAK3 autophosphorylation. Kirken, R.A., et al. "Tyrphostin AG-490 inhibits cytokine-mediated JAK3/STAT5a/b signal transduction and cellular proliferation of antigen-activated human T cells." J. Leukoc. Biol. 65: 891-899 (1999). Wang, L.H., 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." J. Immunol. 162: 3897-3904 (1999). De Vos, J., et al. "JAK2 tyrosine kinase inhibitor tyrphostin AG490 downregulates the mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription (STAT) pathways and induces apoptosis in myeloma cells." Br. J. Haematol. 109: 823-828 (2000).
• Previously sold as "Tyrphostin B42"; the catalog number has not changed.
• Please request Technical Note #22 for additional information.
• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

Related Terms:

Storage

Solubility

Disposal