CBL0137 是一种代谢稳定的 curaxin，可激活 p53 (EC50: 0.37 μM) 并抑制 NF-Κb (EC50: 0.47 μM)。它在功能上使促进染色质转录复合物 (FACT) 失活，从而驱动对 p53 和 NF-Κb 的影响并促进癌细胞死亡。口服 CBL0137 在小鼠体内具有广泛的抗癌活性，可根除耐药性癌症干细胞，并增强吉西他滨在胰腺癌临床前模型中的疗效。

CBL0137, a metabolically stable curaxin, activates p53 (EC50: 0.37 μM) and inhibits NF-κB (EC50: 0.47 μM). It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates the efficacy of gemcitabine in preClinicalal models of pancreatic cancer.

1197996-80-7

C21H24N2O2

336.435

CBLC137;Curaxin 137

H2O:Insoluble
DMSO:~5 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years