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]. Animal Model: SCID mice with RPMI-8226 cells[1] Dosage: 31.25, 62.5, 125 mg/kg Administration: Oal administration; 5 times weekly (31.25 and 62.5 mg/kg), 3 times weekly (125 mg/kg); 2 weeks Result: Showed statistically significant tumor growth inhibition at dose levels of 62.5 mg/kg or 125 mg/kg.
In Vitro
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]. Cell Viability Assay[1] Cell Line: MM.1S cells, RPMI-8226 cells Concentration: 0.01, 0.1, 10 μM Incubation Time: 72 hours Result: Suppressed the growth of a variety of cancer cell lines and the estimated IC50 values ranged from 22.3 or 35.6 nM in MM.1S or RPMI-8226 cells. Western Blot Analysis[1] Cell Line: MM.1S cells Concentration: 1, 3, 6, 12, 25, 50, 100, 200, 400 nM Incubation Time: 24 hours Result: The level of CRM1 protein expression markedly reduced in a dose-dependent manner.
Kinase Assay
Cell Assay
Animal Administration
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.
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