Dual inhibitor of Abl and Src kinases (IC50= 1.2 nM for Src in an enzymatic assay). Displays antiproliferative activity against chronic myelogenous leukemia (CML) cells and decreases the motility and invasion of breast cancer cell lines. Also exhibits pot
Legal Information
Sold for research purposes under agreement from Pfizer Inc. - Not for human or veterinary use.
Shipped In
Normal
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Tyrosine-protein kinase Lyn inhibitor
Product Description
Bosutinib (SKI-606) is a potent c-Abl, Bcr-Abl, and Src-Abl kinase inhibitor, shown to effectively interfere with the progress of chronic myelogenous leukemia (CML). In a competitive study with Imatinib, Bosutinib was shown to inhibit Bcr-Abl kinase activity in CD34+ CML cells more potently than Imatinib. Activity of Src-Abl has been implicated in the development of other non-CML malignancies, and Bosutinib has demonstrated in studies to suppress breast cancer growth and migration. A c-Abl, Src-Abl, and Bcr-Abl inhibitor
1.Puttini M, Coluccia AM, Boschelli F, Cleris L, Marchesi E, Donella-Deana A, Ahmed S, Redaelli S, Piazza R, Magistroni V et al.. (2006) In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells.. Cancer Res, 66 (23):(11314-22). [PMID:17114238]
2.Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Müller A, Baumgartner C, Valent P, Augustin M et al.. (2009) Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.. Leukemia, 23 (3):(477-85). [PMID:19039322]
3.Ozanne J, Prescott AR, Clark K. (2015) The clinically approved drugs dasatinib and bosutinib induce anti-inflammatory macrophages by inhibiting the salt-inducible kinases.. Biochem J, 465 (2):(271-9). [PMID:25351958]
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B1512016