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Tyrphostin AG 957, 5 mg  

Tyrphostin AG 957, 5 mg

4-Amino-N-(2,5-dihydroxybenzyl)methyl benzoate

Synonyms: AG 957, Tyrphostin AG957, AG-957, NSC 654705, Lavendustin C analogue
potent tyrosine kinase inhibitor which selectively blocks the tyrosine kinase activity of human bcr-abl

More details

PKI-AG957-005

Availability: within 3 days

215,00 €

Background: Tyrphostin AG 957 is a a potent tyrosine kinase inhibitor which selectively blocks the tyrosine kinase activity of human bcr-abl (Ki ~ 750 nM) over c-abl (Ki ~ 10 µM). It also decreases bcr-abl phosphorylation in viable K562 cells at concentrations and durations of exposure that also inhibit cell proliferation. It has been reported to alter the physical state of bcr-abl and the association of bcr-abl with Shc and Grb2 in K562 cells.

Chemical formula: C15H15NO4
Molecular weight: 273.3 g/mol
Purity: >98%
Appearance: Off-white solid, Protect from light
Solubility: soluble in DMSO

Product specific literature references:

Anafi M, Gazit A, Gilon C, Ben-Neriah Y, Levitzki A (1992) "Selective interactions of transforming and normal abl proteins with ATP, tyrosine-copolymer substrates, and tyrphostins" J Biol Chem. 1992 Mar 5;267(7):4518-23

Kaur G, Gazit A, Levitzki A, Stowe E, Cooney DA, Sausville EA (1994) "Tyrphostin induced growth inhibition: correlation with effect on p210bcr-abl autokinase activity in K562 chronic myelogenous leukemia" Anticancer Drugs. 5(2):213-22

Bhatia R, Munthe HA, Verfaillie CM (1998) "Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in chronic myelogenous leukemia hematopoietic progenitors" Leukemia 12(11):1708-17

Carlo-Stella C, Regazzi E, Rizzoli V et al (1999) "Effects of the tyrosine kinase inhibitor AG957 and an Anti-Fas receptor antibody on CD34(+) chronic myelogenous leukemia progenitor cells" Blood. 93(11):3973-82

Losiewicz MD, Kaur G, Sausville EA (1999) "Different early effets of tyrphostin AG957 and geldanamycins on mitogen-activated protein kinase and p120cbl phosphorylation in anti CD-3-stimulated T-lymphoblasts" Biochem Pharmacol. 57(3):281-9

Svingen PA, Tefferi A, Kaufmann SH et al (2000) "Effects of the bcr/abl kinase inhibitors AG957 and NSC 680410 on chronic myelogenous leukemia cells in vitro" Clin Cancer Res. 6(1):237-49

Sun X, Layton JE, Elefanty A, Lieschke GJ (2001) "Comparison of effects of the tyrosine kinase inhibitors AG957, AG490, and STI571 on BCR-ABL--expressing cells, demonstrating synergy between AG490 and STI571" Blood. 97(7):2008-15

Urbano A, Gorgun G, Foss F (2002) "Mechanisms of apoptosis by the tyrphostin AG957 in hematopoietic cells" Biochem Pharmacol. 63(4):689-92

Kaur G, Narayanan VL, Sausville EA (2005) "Synthesis, structure-activity relationship, and p210(bcr-abl) protein tyrosine kinase activity of novel AG 957 analogs" Bioorg Med Chem. 13(5):1749-61

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.