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GENTAUR
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T-9142 Tyrphostin AG 490, >99%
[AG 490] [Tyrphostin B42] [N-Benzyl-3,4-dihydroxy-benzylidenecyanoacetamide]
| M.W. 294.31 |
C17H14N2O3
|
[134036-52-5] |
Storage: Store at or below -20 ºC. Solubility: Soluble in
DMSO. Appearance: Cream solid. 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. "Tyrosine phosphorylation is an obligatory event in IL-2
secretion." 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.
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| Please request Technical Note #22 for additional information. |
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