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Bosutinib

Chemical Structure : Bosutinib

CAS No.: 380843-75-4

Bosutinib (SKI-606, SKI 606)

Catalog No.: PC-24042Not For Human Use, Lab Use Only.

Bosutinib (SKI-606) is a potent, dual Src/Abl inhibitor with IC50 of 1.2 nM (Src enzyme), inhibits Src autophosphorylation with an IC50 of 0.25 uM in HT29 cells, inhibits bacterially expressed Abl kinase activity with IC50 of 1 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Bosutinib (SKI-606) is a potent, dual Src/Abl inhibitor with IC50 of 1.2 nM (Src enzyme), inhibits Src autophosphorylation with an IC50 of 0.25 uM in HT29 cells, inhibits bacterially expressed Abl kinase activity with IC50 of 1 nM.
Bosutinib (SKI-606) inhibits the growth of the Abl-MLV-transformed fibroblasts with IC50 of 90 nM
Bosutinib (SKI-606) inhibits v-Abl phosphorylation with IC50 of 25-50 nM, inhibits STAT5 Phosphorylation.
Bosutinib (SKI-606) inhibits anchorage-independent growth of Src-transformed fibroblasts with an IC50 of 100 nM, and inhibits Src-dependent protein tyrosine phosphorylation.
Bosutinib (SKI-606) inhibits proliferation in CML cells, inhibits tyrosine phosphorylation of cellular proteins and Bcr-Abl in CML cells.
Bosutinib (SKI-606) displays excellent antitumor activity in Src-transformed fibroblast xenografts in nude mice.

Physicochemical Properties

M.Wt 530.45
Formula C26H29Cl2N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

References

1. Golas JM, et al. Cancer Res. 2003 Jan 15;63(2):375-81.

2. Golas JM, et al. Cancer Res. 2005 Jun 15;65(12):5358-64.

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