CBL0137

CBL0137 是一种 curaxin 化合物，是一种组蛋白伴侣促进染色质转录 (FACT) 抑制剂。CBL0137 下调 NF-?B 并激活 p53。CBL0137 可恢复组蛋白 H3 乙酰化和三甲基化。CBL0137 是一种抗癌剂。CBL0137 诱导癌细胞凋亡 (apoptosis)。

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5mg

￥785.00

550.00

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10mg

￥1428.00

1000.00

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￥2134.00

1500.00
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￥3571.00

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货号: ajci13510
CAS: 1197996-80-7
别名: CBLC137,Curaxin 137
分子式: C21H24N2O2
分子量: 336.4
纯度: ＞99%
溶解度: ≤2mg/ml in ethanol;5mg/ml in DMSO;5mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

EC50: 0.37 μM for activating p53; 0.47 μM for inhibiting NF-κB

CBL0137 is a curaxin that activates p53 and inhibits NF-κB.

The p53 and nuclear factor κB (NF-κB) pathways are dysregulated in almost all tumors, making them attractive targets for therapeutic activation and inhibition, respectively.

In vitro: CBL0137 was identified as a metabolically stable curaxin activating p53 and inhibiting NF-κB. CBL0137 could functionally inactivate chromatin transcription complex, resulting in the effects on p53 and NF-κB and promoting cancer cell death [1]. It was also found that CBL0137 alone was a potent inducer of apoptosis in pancreatic cancer cell lines and was toxic not only for proliferating bulk tumor cells, but also for pancreatic cancer stem cells [2].

In vivo: 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 [2].

Clinical trial: A phase 1 trial of CBL0137 in patients with metastatic or unresectable advanced solid neoplasm and a study of IV CBL0137 in previously treated hematological subjects are crrently recruiting patients [https://clinicaltrials.gov/ct2/results term=CBL0137&Search=Search].

参考文献:
1.? A. V. Gasparian, C. A. Burkhart, A. A. Purmal, et al. Curaxins: Anticancer compounds that simultaneously suppress NF-κB and activate p53 by targeting FACT. Sci.Transl.Med. 3(95), (2011).
2.? C. Burkhart, D. Fleyshman, R. Kohrn, et al. Curaxin CBL0137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer. Oncotarget 5(22), 11038-11053 (2014).