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- 详细信息
- 文献和实验
- 技术资料
- 库存:
51
- 英文名:
CBL0137
- CAS号:
1197996-80-7
- 供应商:
上海莼试
- 保存条件:
Store at -20°C
- 规格:
1mg 5mg 10mg
| 货号 | CS-01Y65463 | 规格 | 1mg 5mg 10mg |
| CAS号 | 1197996-80-7 | 分子量 | 336.4 |
| 含量 | >98.00% | 别名 | CBLC137,Curaxin 137 |
| 分子式 | C21H24N2O2 | 化学名 | 1,1'-[9-[2-[(1-methylethyl)amino]ethyl]-9H-carbazole-3,6-diyl]bis-ethanone |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C21H24N2O2

分子量:336.4
溶解度:≤2mg/ml in ethanol;5mg/ml in DMSO;5mg/ml in dimethyl formamide
储存条件: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
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 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).
注意事项:
抗逆滴加序列
每次向板内滴加抗原时,移液器滴头要与平面45度悬空,不要触碰到孔内的液体,由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下,必须反应30min以上,若环境温度低于室温,可将微量反应板置于恒温培养箱中,使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定,往往在高压后pH值会有所改变,所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时,红细胞会产生自凝现象;当pH>7.8时,图形洗脱加快,易造成肉眼观察产生误差;p H=7.2时,红细胞沉降最充分,图形最清晰。
当滴注 1%红细胞悬液时,应经常摇晃红细胞悬液,使红细胞均匀地分布在磷酸缓冲液中,以防止红细胞下降。
反应时间及温度
加入鸡红血球之后,反应板在室温(20~25℃)静置30~40min,对照孔血球下沉于孔底,即可判定结果。若室温达不到实验要求,需相应调整反应时间。当环境温度低于4℃时,红细胞发生自凝;高于37℃时,会发生反应物分离和红细胞溶血。
使用方法:
1.本蛋白酶抑制剂混合物为100×的储存液,使用时按照1:100的比例加入到裂解液中(例如,1ml裂解液中加入10μl蛋白酶抑制剂混合物),混匀后即可使用。根据需要,0.5M的EDTA也按照1:100的比例加入到裂解液中(如用于检测金属蛋白酶活性,则不宜添加EDTA)。含有蛋白酶抑制剂混合物的裂解液宜现用现配,不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后,就可以开始进行哺乳动物组织的裂解和蛋白提取。
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): 3044–3048.doi:10.1002/pmic.201200071.Mukhopadhyay, C. et al. (2016). Casitas B-cell lymphoma (Cbl) proteins protect mammary epithelial cells from proteotoxicity of active c-Src accumulation . PNAS 5:8228-8237Wang, J. et al. (2015). Dramatic Improvement
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