CBL0137

SKU: orb1226817

Description

CBL0137 (Curaxin CBL0137) is a histone chaperone FACT (facilitates chromatin transcription) and MYC signal inhibitor that markedly reduced tumor initiation and progression in vivo; simultaneously activates p53 and inhibits NF-κB without causing detectable genotoxicity, causes phosphorylation of p53 Ser(392) by CK2 and inhibition of NF-κB-dependent transcription in neuroblastoma cells; eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer.Brain Cancer Phase 1 Clinical.

Key Properties

• CAS Number: 1197996-80-7
• MW: 336.435
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₄N₂O₂
• SMILES: CC(NCCN1C2=C(C3=C1C=CC(C(C)=O)=C3)C=C(C(C)=O)C=C2)C
• Target: c-Myc

Bioactivity

• In Vivo:
  The CBL-0137 monotherapy group and the CBL-0137-gemcitabine combination group samples show large necrotic fields, numerous apoptotic bodies and loss of tumor cells. Sub-optimal doses of 50 to 60 mg/kg CBL-0137 causes similar enhancement of gemcitabine antitumor activity as that produced by the maximum tolerated dose (MTD) of 90 mg/kg as indicated by the lack of statistically significant differences among the combination groups. CBL0137 hydrochloride inhibits FACT function through depletion of the pool of active FACT involved in transcription elongation. CBL-0137, given by oral gavage at a nontoxic dose of 30 mg/kg per day on a 5 days on/2 days off schedule, suppresses tumor growth in xenografts of colon (DLD-1), renal cell carcinoma (Caki-1), and melanoma (Mel-7) tumor cell lines and transplanted surgical samples from patients with pancreatic ductal adenocarcinoma.
• In Vitro:
  Treatment with CBL-0137 leads to complete absence of living cells at concentrations above 2.5 μM. CBL-0137 causes a greater reduction in the number of colonies formed of not only MiaPaCa-2 cells when combined with gemcitabine, but also gemcitabine-resistant PANC-1 cells. Treatment of human pancreatic cancer cells with CBL-0137 results in a dose dependent reduction of protein and mRNA levels of RRM1 and RRM2. CBL-0137 is able to prevent gemcitabine induced expression of RRM1 and RRM2 on mRNA and protein levels.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CBL-0137 | CBL 0137 | Curaxin CBL0137 | CBLC 137

Quick Database Links

Gene Symbol

c-Myc