Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C21H24N2O2 |
| Molecular Weight | 336.4275 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)NCCN1C2=CC=C(C=C2C3=C1C=CC(=C3)C(C)=O)C(C)=O
InChI
InChIKey=JKCSODVERGVDLT-UHFFFAOYSA-N
InChI=1S/C21H24N2O2/c1-13(2)22-9-10-23-20-7-5-16(14(3)24)11-18(20)19-12-17(15(4)25)6-8-21(19)23/h5-8,11-13,22H,9-10H2,1-4H3
CBL0137 (also known as Curaxin CBL0137) is a metabolically stable curaxin and belongs to the class of small molecules with anti-cancer activity. CBL0137 is in Phase I clinical trials to treat hematological malignancies and solid tumors. CBL0137 binds to Facilitates Chromatin Transcription (FACT) and sequesters the FACT complex on chromatin, which inhibits its activity. This prevents transcription of certain genes involved in cancer-associated signaling pathways; it specifically inhibits the transcription of both NF-kappa β and heat shock transcription factor 1 (HSF1) and simultaneously activates p53. In addition, CBL0137 was investigated in vitro and in models mice for pancreatic ductal adenocarcinoma (PDA) and the obtained data suggested testing of CBL0137 efficacy in Phase II trial in PDA patients alone and in combination with gemcitabine.
Originator
Approval Year
Sample Use Guides
Dose Level 1: 120mg/m2, IV; dose Level 2: 150mg/m2, IV; dose Level 3: 180mg/m2, IV; dose Level 4: 240mg/m2, IV; dose Level 5: 20mg/m2, IV; dose Level 6: 400mg/m2, IV. All dose are on Days 1 and 8 of every 22 day cycle. Number of Cycles: 2 or until progression or unacceptable toxicity develops.
Route of Administration:
Intravenous
To test the effect of CBL0137 on gemcitabine-sensitive and -resistant Pancreatic ductal adenocarcinoma (PDA) cells, MiaPaCa-2 and PANC-1 human PDA cell lines were used, which are gemcitabine-sensitive and resistant, respectively. Both cell lines were sensitive to CBL0137 in 72h viability assays. Importantly, while treatment with CBL0137 (range of concentration is 0-6 uM) led to complete absence of living cells at concentrations above 2.5 μM, gemcitabine treatment, which as reported was more effective against MiaPaCa-2 than PANC-1 cells, resulted in growth arrest rather than cell death since no reduction in the number of living cells were observed with dose escalation.
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SUBSTANCE RECORD
