CBL0137 (CBL-0137)

Catalog No.S8483 Synonyms: CBLC137, Curaxin 137

CBL0137 (CBL-0137) Chemical Structure

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).
Targets
FACT [1]
()
p53 [1]
(Cell-free assay)
NF-κB [1]
(Cell-free assay)
0.37 μM(EC50) 0.47 μM(EC50)
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].

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:

[1]

+ Expand
  • Cell lines: tumor (HT1080, RCC45, MiaPaca) and normal cells (Wi38, NKE-hTERT)
  • Concentrations: 2 μM
  • Incubation Time: 24 h
  • Method:

    Effects of CBLC137 (2 μM for 24 hours) on cell cycle in tumor (HT1080, RCC45, MiaPaca) and normal cells (Wi38, NKE-hTERT) are examined using FACS analysis of propidium iodide-stained cells.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: xenograft mouse models of cancer (athymic nude mice)
  • Formulation: water
  • Dosages: 30 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 38 mg/mL (101.9 mM)
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
Formula

C21H24N2O2.HCl

CAS No. 1197397-89-9
Storage powder
in solvent
Synonyms CBLC137, Curaxin 137

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID