CBL0137 (CBL-0137)
Catalog No.S8483 Synonyms: CBLC137, Curaxin 137
Molecular Weight(MW): 372.89
CBL0137(CBL-0137) activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).
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Biological Activity
| Description | CBL0137(CBL-0137) activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex). | ||||||
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| In vitro |
CBL0137 is a potent inducer of apoptosis in pancreatic cancer cell lines and is toxic not only for proliferating bulk tumor cells, but also for pancreatic cancer stem cells. CBL0137 and related molecules can simultaneously activate p53 and inhibit cellular stress pathways mediated by NF-κB and HSF-1[2]. CBL0137 binds DNA but does not cause any sort of chemical modifications in DNA and therefore lacks genotoxicity. However, CBL0137 binding to DNA leads to functional inactivation of the Facilitates Chromatin Transcription (FACT) complex, a chromatin remodeling complex involved in transcription, replication, and DNA repair. In CBL0137-treated cells, FACT is lost from the nucleoplasm and trapped in chromatin, resulting in the inhibition of FACT-dependent transcription, including NF-kB-mediated transcription. Additionally, chromatin trapping of FACT leads to casein kinase 2 (CK2)-dependent phosphorylation and activation of p53[3]. |
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| In vivo | In mice, CBL0137 is effective against several Pancreatic ductal adenocarcinoma (PDA) models, including orthotopic gemcitabine resistant PANC-1 model and patient derived xenografts, in which CBL0137 anti-tumor effect correlated with overexpression of FACT[1]. CBL0137 targets glioblastoma (GBM) according to its proposed mechanism of action, crosses the blood-brain barrier, and is efficacious in both TMZ-responsive and -resistant orthotopic models. The property of crossing the blood-brain barrier, especially when administered i.v, bodes well for the potential of this drug to treat CNS tumors. In orthotopic models, i.v. administration leads to greater tumor tissue accumulation than oral dosing, leading to greater bioavailability. Normal brain tissue accumulation of CBL0137 does not cause observable neurotoxicity[3]. |
Protocol
| Cell Research: |
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Solubility (25°C)
| In vitro | DMSO | 38 mg/mL (101.9 mM) |
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| Water | 24 mg/mL (64.36 mM) | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 372.89 |
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| Formula | C21H24N2O2.HCl |
| CAS No. | 1197397-89-9 |
| Storage | powder |
| in solvent | |
| Synonyms | CBLC137, Curaxin 137 |
Bio Calculators
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03727789 | Not yet recruiting | Advanced Cutaneous Melanoma of the Extremity|Advanced Sarcoma of the Extremity|Clinical Stage III Cutaneous Melanoma AJCC v8|Clinical Stage IV Cutaneous Melanoma AJCC v8|Pathologic Stage IIIB Cutaneous Melanoma AJCC v8|Pathologic Stage IIIC Cutaneous Melanoma AJCC v8|Pathologic Stage IV Cutaneous Melanoma AJCC v8|Recurrent Cutaneous Melanoma of the Extremity|Recurrent Sarcoma of the Extremity|Stage III Soft Tissue Sarcoma of the Trunk and Extremities AJCC v8|Stage IIIA Soft Tissue Sarcoma of the Trunk and Extremities AJCC v8|Stage IIIB Soft Tissue Sarcoma of the Trunk and Extremities AJCC v8|Stage IV Soft Tissue Sarcoma of the Trunk and Extremities AJCC v8 | Roswell Park Cancer Institute|National Cancer Institute (NCI)|Incuron | April 28 2019 | Phase 1 |
| NCT03727789 | Not yet recruiting | Advanced Cutaneous Melanoma of the Extremity|Advanced Sarcoma of the Extremity|Clinical Stage III Cutaneous Melanoma AJCC v8|Clinical Stage IV Cutaneous Melanoma AJCC v8|Pathologic Stage IIIB Cutaneous Melanoma AJCC v8|Pathologic Stage IIIC Cutaneous Melanoma AJCC v8|Pathologic Stage IV Cutaneous Melanoma AJCC v8|Recurrent Cutaneous Melanoma of the Extremity|Recurrent Sarcoma of the Extremity|Stage III Soft Tissue Sarcoma of the Trunk and Extremities AJCC v8|Stage IIIA Soft Tissue Sarcoma of the Trunk and Extremities AJCC v8|Stage IIIB Soft Tissue Sarcoma of the Trunk and Extremities AJCC v8|Stage IV Soft Tissue Sarcoma of the Trunk and Extremities AJCC v8 | Roswell Park Cancer Institute|National Cancer Institute (NCI)|Incuron | April 28 2019 | Phase 1 |
| NCT02931110 | Recruiting | Hematological Malignancies | Incuron | January 2017 | Phase 1 |
| NCT02931110 | Recruiting | Hematological Malignancies | Incuron | January 2017 | Phase 1 |
| NCT01905228 | Recruiting | Solid Tumors|Glioblastoma | Incuron | July 2013 | Phase 1 |
| NCT01905228 | Recruiting | Solid Tumors|Glioblastoma | Incuron | July 2013 | Phase 1 |
Tech Support
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