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.
Compound Libraries
Bosutinib is also offered as part of the Tocriscreen Plus, Tocriscreen Kinase Inhibitor Toolbox II and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 530.45 |
| Formula | C26H29Cl2N5O3 |
| Storage | Store at +4°C |
| Purity | ≥99% |
| CAS Number | 380843-75-4 |
| PubChem ID | 5328940 |
| InChI Key | UBPYILGKFZZVDX-UHFFFAOYSA-N |
| Smiles | ClC1=CC(Cl)=C(OC)C=C1NC3=C(C#N)C=NC2=CC(OCCCN4CCN(C)CC4)=C(OC)C=C23 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.05 | 100 | |
| ethanol | 13.26 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 530.45. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
Boschelli et al (2001) Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J.Med.Chem. 44 3965 PMID: 11689083
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
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
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
Keywords: Bosutinib, supplier, dual, inhibitors, inhibits, abl, src, kinases, antiproliferative, SKI-606, Src, Kinases, Abl, Kinase, Src, Kinases, Tocris Bioscience
