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Cat. No. Name Size Price Add Cart
KI0319Bosutinib10 mg$112
Bosutinib50 mg$432

Chemical Characteristic

Product NameBosutinib
SynonymsSKI-606
CAS No.380843-75-4
Molecular Weight 530.45
FormulaC26H29Cl2N5O3
Chemical Name4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile
Smilesn1cc(c(c2cc(c(cc12)OCCCN1CCN(CC1)C)OC)Nc1c(cc(c(c1)OC)Cl)Cl)C#N
Chemical Structure

Biological activities

Bosutinib is a novel orally active, competitive inhibitor of both Src and Abl tyrosine kinases with IC50 values of 1.2 nM and 1.4 nM, respectively. [1] Bosutinib inhibited Src-related kinase Fgr, Lyn and Csk with IC50s of 0.174, 0.850, 314 nM, respectively.[3] Bosutinib is a potent antiproliferative and proapoptotic agent in chronic myelogenous leukemia (CML) cells and inhibits Bcr-Abl mediated signaling at nanomolar concentrations. Bosutinib inhibits chromosome-positive cell lines KU812 with an IC50 of 5 nM. Short-term administration of bosutinib causes regression of K562 and KU812 CML tumor xenografts. BaF3 murine myeloid cells expressing wild-type Bcr-Abl are sensitive to bosutinib treatment, as are BaF3 cells expressing many imatinib-resistant forms of Bcr-Abl. Bosutinib also inhibits the multidrug transport proteins at concentrations greater than 1 μM, thus, bosutinib can be accumulated in tumor tissue. Bosutinib does inhibit EGFR enzyme activity with an IC50 of about 350 nM, and is able to reduce EGFR autophosphorylation (Y1068) or the levels of ??ctivated??EGFR in cells with an IC50 between 0.5 and 1 μM. [1] Bosutinib dose-dependently reduces the activation of Src, proliferation and migration of the highly invasive human prostate cancer cells PC-3 and DU-145, as well as their invasion. Bosutinib treatment results in a significant (80%) decrease in tumor volume in xenograft -bearing mice. [2]

Protocols

Bosutinib is prepared at 1 and 10 mM in DMSO filtered, and stores at -20°C.[3]

References

[1] Boschelli F, et al. Bosutinib: A review of preclinical studies in chronic myelogenous leukaemia. Eur J Cancer. 2010, 46: 1781-1789.
[2] Rabbani SA, et al. SKI-606 (Bosutinib) Blocks Prostate Cancer Invasion, Growth, and Metastasis In vitro and In vivo through Regulation of Genes Involved in Cancer Growth and Skeletal Metastasis. Mol Cancer Ther. 2010, 9(15): 1147-1157.
[3] Miriam P, et al. In vitro and in vivo Activity of SKI-606, a Novel Src-Abl Inhibitor, against Imatinib-Resistant Bcr-Abl+ Neoplastic Cells. Cancer Res 2006, 66, 11314-11322.

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