CBS9106 (BMS566419) Chemical Properties,Usage,Production
Uses
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].
in vivo
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.
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. DOI:10.1182/blood-2011-01-333138