AG957

• CAT Number: I011475
• CAS Number: 140674-76-6
• Molecular Formula: C15H15NO4
• Molecular Weight: 273.28
• Purity: ≥95%
• Synonyms: methyl 4-[(2,5-dihydroxyphenyl)methylamino]benzoate
• InChI: InChI=1S/C15H15NO4/c1-20-15(19)10-2-4-12(5-3-10)16-9-11-8-13(17)6-7-14(11)18/h2-8,16-18H,9H2,1H3
• InChIKey: QSFREBZMBNRGOK-UHFFFAOYSA-N
• SMILES: COC(=O)C1=CC=C(C=C1)NCC2=C(C=CC(=C2)O)O

AG957 (Cat No.: I011475) is a small-molecule tyrosine kinase inhibitor that selectively targets the Bcr-Abl fusion protein, a constitutively active kinase implicated in chronic myelogenous leukemia (CML). By inhibiting Bcr-Abl signaling, AG957 suppresses leukemic cell proliferation and promotes apoptosis. Although it was not advanced to clinical use, AG957 served as an early prototype for later Abl kinase inhibitors such as imatinib. It remains a valuable research tool for studying oncogenic kinase signaling, leukemia biology, and the development of targeted cancer therapies.

Reference

[1]. G Kaur, et al. Tyrphostin induced growth inhibition: correlation with effect on p210bcr-abl autokinase activity in K562 chronic myelogenous leukemia. Anticancer Drugs. 1994 Apr;5(2):213-22.
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[2]. R Bhatia, et al. 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. 1998 Nov;12(1
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[3]. P A Svingen, et al. Effects of the bcr/abl kinase inhibitors AG957 and NSC 680410 on chronic myelogenous leukemia cells in vitro. Clin Cancer Res. 2000 Jan;6(1):237-49.
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[4]. Panfeng Fu, et al. c-Abl mediated tyrosine phosphorylation of paxillin regulates LPS-induced endothelial dysfunction and lung injury. Am J Physiol Lung Cell Mol Physiol. 2015 May 15;308(10):L1025-38.
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