Adaphostin is the lipophilic, adamantyl ester of tyrphostin AG 957 that displays antiproliferative properties. It has been demonstrated to be selective and ~ 3-4 fold more potent than the bcr/abl kinase inhibitor tyrphostin AG 957 and has a longer half-life in serum. Adaphostin downregulates bcr/abl autophosphorylation activity (IC50 = 14 µM), selectively blocks granulocyte colony formation in CML (chronic myelogenous leukemia) progenitor cells and inhibits proliferation of K562 cells (IC50 = 9.8 µM) by inducing apoptosis. Molecular weight 393.5 g/mol. Solubility: soluble in DMSO or ethanol. Purity: >97% (HPLC). Handling: Protect from light. Appearance: Off-white solid. Chemical formula C₂₄H₂₇NO₄.

Ordering informations: shipped on blue ice

Product specific literature references:

ASvingen 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

Mow BM, Chandra J, Kaufmann SH et al. (2002) "Effects of the Bcr/abl kinase inhibitors STI571 and adaphostin (NSC 680410) on chronic myelogenous leukemia cells in vitro" Blood 99(2):664-71

Avramis IA, Laug WE, Sausville EA, Avramis VI (2003) "Determination of drug synergism between the tyrosine kinase inhibitors NSC 680410 (adaphostin) and/or STI571 (imatinib mesylate, Gleevec) with cytotoxic drugs against human leukemia cell lines" Cancer Chemother Pharmacol. 52(4):307-18

Yu C, Rahmani M, Grant S et al. (2004) "Induction of apoptosis in human leukemia cells by the tyrosine kinase inhibitor adaphostin proceeds through a RAF-1/MEK/ERK- and AKT-dependent process" Oncogene 23(7):1364-76

Kaur G, Narayanan VL, Sausville EA et al. (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

Shanafelt TD, Lee YK, Kay NE et al. (2005) "Adaphostin-induced apoptosis in CLL B cells is associated with induction of oxidative stress and exhibits synergy with fludarabine" Blood 105(5):2099-106

Price*: EUR 385,00

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This product was added to our catalog on Jan 03, 2007


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