T-9142 Tyrphostin AG 490, >99%

Related Terms : [AG 490] [Tyrphostin B42] [N-Benzyl-3,4-dihydroxy-benzylidenecyanoacetamide]

  • Size
  • US $
  • £
  • ¥
  • 10 mg
  • 42
  • 39
  • 33
  • 4,800
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  • In stock
  • 25 mg
  • 69
  • 64
  • 54
  • 7,900
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  • In stock
  • 50 mg
  • 88
  • 82
  • 69
  • 10,100
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  • In stock
  • 100 mg
  • 115
  • 108
  • 91
  • 13,200
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  • In stock
  • 250 mg
  • 232
  • 218
  • 184
  • 26,500
  • Add to Cart Qty:
  • In stock
  • 300 mg
  • 258
  • 243
  • 204
  • 29,500
  • Add to Cart Qty:
  • In stock
  • 1 g
  • 598
  • 563
  • 474
  • 68,400
  • Add to Cart Qty:
  • In stock

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  • 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. Disposal: A.

  • 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.
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