Felezonexor, also known as CBS9106, SL-801, and BMS566419, is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. CRM1 plays an important role in the nuclear export of cargo proteins bearing nuclear exporting signal sequences. 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, including multiple myeloma cells. CBS9106 reduces CRM1 protein levels significantly without affecting CRM1 mRNA expression. Oral administration of CBS9106 significantly suppresses tumor growth and prolongs survival in mice bearing tumor xenograft without a significant loss in body weight.
CAS 1076235-04-5 MFCD176235045
化学结构图
SMILES: CC1=C(COCCC(C)(C)C)C(=O)N(Nc2ccc(C(F)(F)F)c(Cl)n2)C1=O
化学属性
| Mol. Weight | 419.83 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | Felezonexor, also known as CBS9106, SL-801, and BMS566419, is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. CRM1 plays an important role in the nuclear export of cargo proteins bearing nuclear exporting signal sequences. 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, including multiple myeloma cells. CBS9106 reduces CRM1 protein levels significantly without affecting CRM1 mRNA expression. Oral administration of CBS9106 significantly suppresses tumor growth and prolongs survival in mice bearing tumor xenograft without a significant loss in body weight. |
|---|---|
| Formula | C18H21ClF3N3O3 |
| Synonym | CBS9106; CBS-9106; CBS 9106; SL-801; SL801; SL 801; BMS566419; BMS-566419; BMS 566419; Felezonexor |
| IUPAC Name | 1-((6-chloro-5-(trifluoromethyl)pyridin-2-yl)amino)-3-((3,3-dimethylbutoxy)methyl)-4-methyl-1H-pyrrole-2,5-dione |
| InChIKey | CMASLSTVVOYJQY-UHFFFAOYSA-N |
| InChI | InChI=1S/C18H21ClF3N3O3/c1-10-11(9-28-8-7-17(2,3)4)16(27)25(15(10)26)24-13-6-5-12(14(19)23-13)18(20,21)22/h5-6H,7-9H2,1-4H3,(H,23,24) |
| Canonical SMILES | O=C(C(COCCC(C)(C)C)=C1C)N(NC2=NC(Cl)=C(C(F)(F)F)C=C2)C1=O |
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- Felezonexor, also known as CBS9106, SL-801, and BMS566419, is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. CRM1 plays an important role in the nuclear export of cargo proteins bearing nuclear exporting signal sequences. 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, including multiple myeloma cells. CBS9106 reduces CRM1 protein levels significantly without affecting CRM1 mRNA expression. Oral administration of CBS9106 significantly suppresses tumor growth and prolongs survival in mice bearing tumor xenograft without a significant loss in body weight.
