TYRPHOSTIN B46 Chemical Properties

Boiling point:

621.1±55.0 °C(Predicted)

Density 

1.273±0.06 g/cm3(Predicted)

storage temp. 

Inert atmosphere,Store in freezer, under -20°C

solubility 

DMSO or ethanol: soluble

pka

8.82±0.10(Predicted)

form 

Powder

color 

Light yellow to yellow

Safety Information

Safety Statements 

22-24/25

WGK Germany 

3

MSDS

• Language:English Provider:SigmaAldrich

TYRPHOSTIN B46 Usage And Synthesis

Description

AG-555 is a tyrphostin inhibitor of the EGF receptor (EGFR; IC₅₀ = 0.7 μM). It selectively inhibits EFGR over ErbB2 (IC₅₀ = 35 μM). AG-555 inhibits EGF-dependent growth of HER 14 cells (IC₅₀ = 2.5 μM) as well as the growth of psoriatic keratinocytes isolated from patients with psoriasis when used at concentrations ranging from 1 to 50 μM. It also inhibits Moloney murine leukemia virus (Mo-MuLV) reverse transcriptase activity (IC₅₀ = 10.8 μM) without affecting Mo-MuLV-infected NIH3T3 cell growth (IC₅₀ = 210 μM).

Uses

Inhibitor of EGF receptor kinase activity

Biological Activity

Potent epidermal growth factor receptor (EGFR) kinase inhibitor (IC 50 = 0.7 μ M) that displays 50-fold and >140-fold selectivity over ErbB2 and insulin receptor kinase respectively. Induce G 1 growth arrest selectively in transformed cells (IC 50 values are 6.4 and 9.4 μ M in HPV16-immortalized and normal keratinocytes respectively).

References

[1]. ben-bassat h, rosenbaum-mitrani s, hartzstark z, et al. inhibitors of epidermal growth factor receptor kinase and of cyclin-dependent kinase 2 activation induce growth arrest, differentiation, and apoptosis of human papilloma virus 16-immortalized human keratinocytes. cancer res, 1997, 57(17): 3741-3750.
[2]. kleinberger-doron n, shelah n, capone r, et al. inhibition of cdk2 activation by selected tyrphostins causes cell cycle arrest at late g1 and s phase. exp cell res, 1998, 241(2): 340-351.
[3]. sion-vardy n, vardy d, rodeck u, et al. antiproliferative effects of tyrosine kinase inhibitors (tyrphostins) on human bladder and renal carcinoma cells. j surg res, 1995, 59(6): 675-680.
[4]. seri i, aflalo e, gazit a, et al. tyrphostin ag-555 inhibits early and late stages of moloney murine leukemia virus replication cycle. int j oncol, 1997, 10(6): 1185-1189.

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