Revision 3

#14704Store at -20C

 

Cell Signaling Technology

Orders: 877-616-CELL (2355) [email protected]

Support: 877-678-TECH (8324)

Web: [email protected] cellsignal.com

3 Trask LaneDanversMassachusetts01923USA
For Research Use Only. Not for Use in Diagnostic Procedures.

Background

Tyrphostin AG-490 is a membrane soluble protein tyrosine kinase inhibitor that primarily blocks Jak2 (IC50 = 10 μM) and Jak3 (IC50 = 20 μM) kinases (1,2). Research studies demonstrate that tyrphostin AG-490 inhibits proliferation and expansion of T cells (3). Unlike many other kinase inhibitors, tyrphostin AG-490 does not block a number of lymphocytic tyrosine kinases, such as Lck, Lyn, Btk, Syk, Jak1, Tyk2, or Src kinase (1,4). Additional studies indicate that tyrphostin AG-490 also selectively inhibits the EGFR (IC50 = 2 μM) and ErbB2 (IC50 = 13.5 μM) receptor tyrosine kinases (5).

  1. Meydan, N. et al. (1996) Nature 379, 645-8.
  2. Murakami, K. and Takagi, T. (1999) Pac Symp Biocomput, 171-81.
  3. Wang, L.H. et al. (1999) J Immunol 162, 3897-904.
  4. De Vos, J. et al. (2000) Br J Haematol 109, 823-8.
  5. Gazit, A. et al. (1991) J Med Chem 34, 1896-907.

Molecular Formula

C17H14N2O3

Molecular Weight

294.3 g/mol

Purity

>99%

CAS

134036-52-5

Solubility

Soluble in DMSO at 200mg/ml and EtOH at 16mg/ml.

Storage

Store lyophilized or in solution at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Directions for Use

Tyrphostin AG-490 is supplied as a lyophilized powder. For a 50 mM stock, reconstitute the 10 mg in 679.58 μl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 10-100 μM for 1-24 hr.

Background References

    Cross-Reactivity Key

    H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected

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