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T-3655 Tyrphostin AG 1478, Methanesulfonate Salt, >99%

[AG 1478] [AG 1478 Mesylate] [AG1478] [AG-1478]

M.W. 411.87

C16H14ClN3O2•CH4O3S

[175178-82-2]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO up to about 25 mg/ml; poorly soluble in ethanol or water, but soluble in aqueous Captisol (see below).  Appearance:  White solid.  Disposal:  A

View the MSDS for this product

• Very potent EGF receptor kinase (tyrosine kinase) inhibitor (IC50 = 3 nM).  Very weak on PDGF receptor and HER2-NEU kinases (IC50 >100 µM).  Osherov, N. and Levitzki, A.  "Epidermal-growth-factor-dependent activation of the src-family kinases."  Eur. J. Biochem. 225:  1047-1053 (1994).  Levitzki, A. and Gazit, A.  "Tyrosine kinase inhibition:  an approach to drug development."  Science 267:  1782-1788 (1995).

• Reversibly inhibits (IC50 = 9.8 µM) the rat brain Kv1.5 potassium channel in vitro in a non-protein-tyrosine-kinase-mediated manner.  Choi, B.H., et al.  "Direct inhibition of the cloned Kv1.5 channel by AG-1478, a tyrosine kinase inhibitor."  Am. J. Physiol. Cell Physiol. 282:  C1461-C1468 (2002).

• Formulations for in vivo use.  This product, the methanesulfonate (mesylate) salt of Tyrphostin AG 1478, can be conveniently formulated as a water-soluble complex with Captisol (β-cyclodextrin hepta-sulfobutyl ether).  Captisol is available from Cydex (Lenexa, Kansas).  Further details about Captisol solutions of Tyrphostin AG 1478 mesylate can be found in:
  --Proc. Natl. Acad. Sci. USA 100:  15871-15876 (2003)  Various concentrations of AG 1478 mesylate were dissolved in 100 mM Captisol for administration to mice via s.c., and i.p. injections.
  --Biochem. Pharmacol. 71:  1422-1434 (2006)  AG 1478 mesylate in Captisol was administered to mice by s.c. injection and to rats by i.v. injection.
  --Anal. Biochem. 42:  292-299 (2005)  These workers used 49 mM AG 1478 mesylate and 49 mM Captisol in aqueous solution to study the in vitro association of this drug with albumin.
  --Clin. Cancer Res. 11:  7080s-7086s (2005)  Here, AG 1478 mesylate at 4 mg/mL was dissolved in 100 mM Captisol and administered to nude mice by i.p. injection.

• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.