Bosutinib

Product Description

Bosutinib is a 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.

Solubility

Preparing Stock Solutions for Bosutinib

The following data is based on the product molecular weight 530.45

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.89 mL	9.43 mL	18.85 mL
5 mM	0.38 mL	1.89 mL	3.77 mL
10 mM	0.19 mL	0.94 mL	1.89 mL
50 mM	0.04 mL	0.19 mL	0.38 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Vultur SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells. Mol.Cancer.Ther. 2008 PMID: 18483306
• Golas 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. 2003 PMID: 12543790
• Golas SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res. 2005 PMID: 15958584
• Boschelli Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J.Med.Chem. 2001 PMID: 11689083