1076235-04-5
| Name | CBS9106 (BMS566419) |
| MDL Number | MFCD28502170 |
| MOL File | 1076235-04-5.mol |
Synonyms
SL-801
S-03747
CBS-9106
CBS9106 (BMS566419)
Felezonexor，CBS9106
1-[[6-chloro-5-(trifluoromethyl)pyridin-2-yl]amino]-3-(3,3-dimethylbutoxymethyl)-4-methylpyrrole-2,5-dione
1-((6-chloro-5-(trifluoromethyl)pyridin-2-yl)amino)-3-((3,3-dimethylbutoxy)methyl)-4-methyl-1H-pyrrole-2,5-dione
1H-Pyrrole-2,5-dione, 1-[[6-chloro-5-(trifluoromethyl)-2-pyridinyl]amino]-3-[(3,3-dimethylbutoxy)methyl]-4-methyl-
Hazard Information
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
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