Bosutinib

Cat. No. 4361

Bosutinib C26H29Cl2N5O3 [380843-75-4]

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Alternative Name: SKI-606

Chemical Name: 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile

Biological Activity

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 potent antiproliferative activity in anchorage-independent, Src-transformed rat fibroblasts (IC50 = 100 nM). Displays selectivity for Src over non-Src family kinases such as growth factor receptor tyrosine kinases.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
530.45
Formula:
C26H29Cl2N5O3
Solubility:
Soluble to 100 mM in DMSO and to 25 mM in ethanol
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
380843-75-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Vultur et al (2008) SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells. Mol.Cancer.Ther. 7 1185. PMID: 18483306.

Golas et al (2005) SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res. 65 5358. PMID: 15958584.

Golas et al (2003) SKI-606, a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiproliferative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice. Cancer Res. 63 375. PMID: 12543790.

Boschelli et al (2001) Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J.Med.Chem. 44 3965. PMID: 11689083.

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Keywords: Bosutinib, supplier, dual, inhibitors, inhibits, abl, src, kinases, antiproliferative, Tocris Bioscience, Src Kinase Inhibitor products

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