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T-9142 Tyrphostin AG 490, >99%

[AG 490] [Tyrphostin B42] [N-Benzyl-3,4-dihydroxy-benzylidenecyanoacetamide] [AG490] [AG-490]

M.W. 294.30

C17H14N2O3

[134036-52-5]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 200 mg/mL; soluble in ethanol at 16 mg/mL; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Appearance:  Cream solid.  Disposal:  A

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• 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.