AG 99 Chemical Properties

Melting point:

247 °C

Boiling point:

544.4±50.0 °C(Predicted)

Density 

1.482±0.06 g/cm3(Predicted)

storage temp. 

Inert atmosphere,Room Temperature

solubility 

Soluble in DMSO

form 

Brown solid.

pka

8.81±0.10(Predicted)

AG 99 Usage And Synthesis

Uses

Tyrphostin AG 99 is a potent, cell-permeable and reversible inhibitor of EGFR and EGF-dependent cell proliferation.

Biological Activity

Epidermal growth factor receptor (EGFR) kinase inhibitor (IC 50 = 10 μ M) that is selective over insulin receptor kinase. Blocks tyrosine phosphorylation of p145 met and promotes cell death of normal and cancer cells via activation of caspase-like proteases in vitro .

References

[1]. gazit a, osherov n, gilon c, et al. tyrphostins. 6. dimeric benzylidenemalononitrile tyrophostins: potent inhibitors of egf receptor tyrosine kinase in vitro. j med chem, 1996, 39(25): 4905-4911.
[2]. yamamoto n, mammadova g, song rx, et al. tyrosine phosphorylation of p145met mediated by egfr and src is required for serum-independent survival of human bladder carcinoma cells. j cell sci, 2006, 119(pt 22): 4623-4633.

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