CBS9106 (SL-801)
CBS9106, also known as SL-801, 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.
1: Gravina G, Senapedis W, McCauley D, Baloglu E, Shacham S, Festuccia C. Nucleo-cytoplasmic transport as a therapeutic target of cancer. J Hematol Oncol. 2014 Dec 5;7(1):85. [Epub ahead of print] PubMed PMID: 25476752.
2: Saito N, Sakakibara K, Sato T, Friedman JM, Kufe DW, VonHoff DD, Kawabe T. CBS9106-Induced CRM1 Degradation Is Mediated by Cullin Ring Ligase Activity and the Neddylation Pathway. Mol Cancer Ther. 2014 Dec;13(12):3013-23. doi: 10.1158/1535-7163.MCT-14-0064. Epub 2014 Sep 24. PubMed PMID: 25253782.
3: Turner JG, Dawson J, Sullivan DM. Nuclear export of proteins and drug resistance in cancer. Biochem Pharmacol. 2012 Apr 15;83(8):1021-32. doi: 10.1016/j.bcp.2011.12.016. Epub 2011 Dec 20. Review. PubMed PMID: 22209898.
4: Sakakibara K, Saito N, Sato T, Suzuki A, Hasegawa Y, Friedman JM, Kufe DW, Vonhoff DD, Iwami T, Kawabe T. 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. Epub 2011 Aug 12. PubMed PMID: 21841164.
2: Saito N, Sakakibara K, Sato T, Friedman JM, Kufe DW, VonHoff DD, Kawabe T. CBS9106-Induced CRM1 Degradation Is Mediated by Cullin Ring Ligase Activity and the Neddylation Pathway. Mol Cancer Ther. 2014 Dec;13(12):3013-23. doi: 10.1158/1535-7163.MCT-14-0064. Epub 2014 Sep 24. PubMed PMID: 25253782.
3: Turner JG, Dawson J, Sullivan DM. Nuclear export of proteins and drug resistance in cancer. Biochem Pharmacol. 2012 Apr 15;83(8):1021-32. doi: 10.1016/j.bcp.2011.12.016. Epub 2011 Dec 20. Review. PubMed PMID: 22209898.
4: Sakakibara K, Saito N, Sato T, Suzuki A, Hasegawa Y, Friedman JM, Kufe DW, Vonhoff DD, Iwami T, Kawabe T. 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. Epub 2011 Aug 12. PubMed PMID: 21841164.
| Chemical | |
|---|---|
| CAS Num | 1076235-04-5 |
| Chemical Formula | C18H21ClF3N3O3 |
| Molecular Weight | 419.83 |
| IUPAC Chemical Name | 1-((6-chloro-5-(trifluoromethyl)pyridin-2-yl)amino)-3-((3,3-dimethylbutoxy)methyl)-4-methyl-1H-pyrrole-2,5-dione |
| Exact Mass | 419.12235 |
| Elemental Analysis | C, 51.50; H, 5.04; Cl, 8.44; F, 13.58; N, 10.01; O, 11.43 |
| Synonym | CBS9106; CBS-9106; CBS 9106; SL-801; SL801; SL 801. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(C(COCCC(C)(C)C)=C1C)N(NC2=NC(Cl)=C(C(F)(F)F)C=C2)C1=O |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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