Bosutinib

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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%
Datasheet
Citations (4)
Reviews

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 Data 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.

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

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


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Keywords: Bosutinib, Bosutinib supplier, dual, inhibitors, inhibits, abl, src, kinases, antiproliferative, SKI-606, Src, Kinases, Abl, Kinase, 4361, Tocris Bioscience

4 Citations for Bosutinib

Citations are publications that use Tocris products. Selected citations for Bosutinib include:

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

Mark et al (2013) Calcium-activated chloride channel ANO1 promotes breast cancer progression by activating EGFR and CAMK signaling. Proc Natl Acad Sci U S A 110 E1026-34 PMID: 23431153

Levinson (2014) A conserved water-mediated hydrogen bond network defines bosutinib's kinase selectivity. Nat Chem Biol 10 127 PMID: 24292070

Marina et al (2021) Machine learning identifies molecular regulators and therapeutics for targeting SARS-CoV2-induced cytokine release. Mol Syst Biol 17 e10426 PMID: 34486798


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