Bosutinib

Name: Bosutinib
Brand: Tocris Bioscience
SKU: 4361

Tocris Bioscience a Bio-Techne Brand

Catalog # 4361

Citations (2)

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Key Product Details

Description:	Dual Src-Abl inhibitor; antiproliferative
Alternative Names:	SKI-606
Chemical Name:	4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile
Purity:	≥99%
Molecular Weight:	530.45

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Biological Activity for Bosutinib

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.

Compound Libraries for Bosutinib

Bosutinib is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Bosutinib

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Bosutinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	53.05	100
	ethanol	13.26	25

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 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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References for Bosutinib

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 Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res. 2005 PMID: 15958584
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
Boschelli Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J.Med.Chem. 2001 PMID: 11689083

Citations for Bosutinib (2)

Showing 1 - 2 of 2 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for Bosutinib include:

Levinson (2014) A conserved water-mediated hydrogen bond network defines bosutinib's kinase selectivity. Nat Chem Biol. 10:127
PMID: 24292070
Levinson and Boxer (2012) Structural and spectroscopic analysis of the kinase inhibitor bosutinib and an isomer of bosutinib binding to the Abl tyrosine kinase domain. PLoS One. 7:e29828
PMID: 22493660

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