1076235-04-5
1076235-04-5 structure
- Name: CBS9106
- Chemical Name: 1-{[6-Chloro-5-(trifluoromethyl)-2-pyridinyl]amino}-3-[(3,3-dimethylbutoxy)methyl]-4-methyl-1H-pyrrole-2,5-dione
- CAS Number: 1076235-04-5
- Molecular Formula: C18H21ClF3N3O3
- Molecular Weight: 419.83
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2018-07-21 11:33:24
- Modify Date: 2024-01-10 16:25:17
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CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities[1].
| Name | 1-{[6-Chloro-5-(trifluoromethyl)-2-pyridinyl]amino}-3-[(3,3-dimethylbutoxy)methyl]-4-methyl-1H-pyrrole-2,5-dione |
|---|---|
| Synonyms |
1-{[6-Chloro-5-(trifluoromethyl)-2-pyridinyl]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- |
| Description | CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities[1]. |
|---|---|
| Related Catalog | |
| Target |
CRM1[1] |
| 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. |
| 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 |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 464.5±55.0 °C at 760 mmHg |
| Molecular Formula | C18H21ClF3N3O3 |
| Molecular Weight | 419.83 |
| Flash Point | 234.7±31.5 °C |
| Exact Mass | 419.122345 |
| LogP | 5.10 |
| Vapour Pressure | 0.0±1.1 mmHg at 25°C |
| Index of Refraction | 1.540 |
| Storage condition | 2-8℃ |