CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM. CBL0137 inhibits histone chaperone FACT, is efficacious in preclinical orthotopic models of temozolomide-responsive and -resistant glioblastoma. CBL0137 eradicates d rug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer.
In mice, CBL0137 was effective against orthotopic gemcitabine resistant PANC-1 model and patient derived xenografts, in which CBL0137 anti-tumor effect related with overexpression of FACT. Moreover, the combination effects of CBL0137 and gemcitabine might be explained by the ability of CBL0137 to inhibit several transcriptional programs induced by gemcitabine, including NF-kappaB response and expression of ribonucleotide reductase.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 10 mM|
Initial testing (stage 1) of the curaxin CBL0137 by the pediatric preclinical testing program.
Lock R, et al. Pediatr Blood Cancer. 2017 Apr;64(4). PMID: 27650817.
Curaxin CBL0137 eradicates d rug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer.
Burkhart C, et al. Oncotarget. 2014 Nov 30;5(22):11038-53. PMID: 25402820.
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