CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells[1].
CBS9106 (0.01-10 μM; 72 hours) sensitizes cells to radiation and to suppress the growth of a variety of cancer cell lines. The estimated IC50 values range from 22.3 or 35.6 nM in multiple myeloma (MM).1S or RPMI-8226 cells and from 3 to 278 nM in 60 other human cancer cell lines[1].CBS9106 (1-400 nM; 24 hours) decreases CRM1 protein expression levels in a dose-dependent manner[1].
CBS9106 (31.25-62.5 mg/kg for 5 times weekly, 125 mg/kg for 3 times weekly; p.o.; 2 weeks) significantly suppresses tumor growth at dose levels of 62.5 or 125 mg/kg in mice bearing human MM xenograft models[1].
References:
[1]. Sakakibara K, et al. CBS9106 is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. Blood. 2011 Oct 6;118(14):3922-31.