產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
CBL0137 (hydrochloride) | 10 mM * 1 mL in DMSO 2mg 5mg 10mg 25mg 50mg | 1197397-89-9 | EY-Y0165564 |
Cas No.1197397-89-9
別名 CBLC137,Curaxin 137
化學名 1,1'-[9-[2-[(1-methylethyl)imino]ethyl]-9H-carbazole-3,6-diyl]bis-ethanone, monohydrochloride
分子式 C21H24N2O2 ? HCl
分子量 372.9
溶解度 ≤25mg/ml in DMSO;20mg/ml in dimethyl formamide
儲存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
EC50: 0.37 μM for activating p53; 0.47 μM for inhibiting NF-κB
CBL0137 (hydrochloride) 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].
References:
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).
關鍵字： 1197397-89-9;C21H24N2O2 ? HCl;CBL0137 (hydrochlori;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學、分子生物學和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè)，公司自成立以來，秉承""全心全意服務于科研工作者""的企業(yè)理念，立足生物科技領域，運用生物技術和科研試劑，發(fā)展現(xiàn)代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機構、高等院校、科研院所、企事業(yè)單位提供優(yōu)質的產(chǎn)品，服務生物科技領域的科學研究人員。
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