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Biological Activity:

ML239 is a potent and selective breast cancer stem cell inhibitor with IC50 ~1.16 μM. It displayed greater than 23-fold selective inhibition of the breast CSC-like cell line (HMLE_sh_Ecad) over the isogenic control cell line (HMLE_sh_GFP). It did not significantly inhibit tumorsphere formation in the breast cancer cell line SUM159, which is a mixture of CSCs and differentiated cells. ML239 is also cytotoxic towards MDA-MB-231 breast cancer cells.

How to Use:

In vitro: ML239 was used at 10 μM final concentration in vitro and in cellular assays.
In vivo: n/a

Reference:

• 1. Carmody LC, et al. Phenotypic high-throughput screening elucidates target pathway in breast cancer stem cell-like cells. (2012) J Biomol Screen. 17(9):1204-10.?
• 2. Germain AR, et al. Identification of a selective small molecule inhibitor of breast cancer stem cells. (2012) Bioorg Med Chem Lett. 22(10):3571-4.
• 3. http://www.ncbi.nlm.nih.gov/books/NBK133423/