Bosutinib, Src/Abl kinase inhibitor

Product Details

Formal Name: 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile

Alternate Names: SKI-606

Molecular Formula: C26H29Cl2N5O3

Formula Weight: 530.60

CAS Number: 380843-75-4

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 25 mg/ml with warming).

Storage: -20°C

Stability: ≥ 2 years.

Applications

Src/Abl kinase inhibitor

Functions

Bosutinib is an ATP-competitive dual Src/Abl kinase inhibitor (IC50 = 1 nM). It potently inhibits the apoptosis-linked STE20 kinases but does not inhibit Kit or PDGFR. Bosutinib was found to inhibit 16 of 18 imatinib-resistant mutant forms of Bcr-Abl expressed in murine myeloid cell lines, but did not inhibit T315I and V299L mutants. Enhances retinoic acid-induced differentiation of HL-60 leukemia cells. Suppresses migration and invasion of human breast cancer cells (IC50 = 250 nM which is also the IC50 for inhibition of cellular Src kinase activity in intact tumor cells).

Application Procedures

First dissolved in DMSO (up to 100 mg/ml) or in Ethanol (up to 25 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 1 month.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)