Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CBL0137 hydrochloride (Curaxin-137 hydrochloride) 是一种组蛋白分子伴侣FACT 的抑制剂,也可激活p53并抑制NF-κB,对于它们的EC50值分别为 0.37 和 0.47 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 396 | 现货 | ||
2 mg | ¥ 578 | 现货 | ||
5 mg | ¥ 1,150 | 现货 | ||
10 mg | ¥ 1,830 | 现货 | ||
25 mg | ¥ 2,970 | 现货 | ||
50 mg | ¥ 4,530 | 现货 | ||
100 mg | ¥ 6,470 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 987 | 现货 |
产品描述 | CBL0137 hydrochloride (Curaxin-137 hydrochloride) activates p53 and inhibits NF-kB (EC50: 0.37/0.47 μM) in the cell-based p53 and NF-kB reporter assays, respectively. It also suppresses histone chaperone FACT. |
靶点活性 | NF-κB:0.47 μM(EC50), p53:0.37 μM(EC50), FACT: |
体外活性 | In pancreatic cancer cell lines, CBL0137 is an effective inducer of apoptosis. It is toxic not only for proliferating various tumor cells, but also for pancreatic cancer stem cells. CBL0137 can activate p53 and inhibit cellular stress pathways mediated by HSF-1 and NF-κB. CBL0137 binds DNA but does not cause any sort of chemical modifications in DNA. However, CBL0137 binding to DNA leads to functional inactivation of the Facilitates Chromatin Transcription (FACT) complex. In CBL0137-treated cells, FACT is lost from the nucleoplasm and trapped in chromatin, resulting in the inhibition of FACT-dependent transcription, including NF-kB-mediated transcription. Additionally, chromatin trapping of FACT leads to casein kinase 2 (CK2)-dependent phosphorylation and activation of p53. |
体内活性 | In mice, CBL0137 is potent against several Pancreatic ductal adenocarcinoma (PDA) models, including patient derived xenografts and orthotopic gemcitabine resistant PANC-1 model. CBL0137 targets glioblastoma (GBM) according to its proposed mechanism of action, crosses the blood-brain barrier, and is efficacious in both TMZ-responsive and -resistant orthotopic models. The property of crossing the blood-brain barrier, especially when administered i.v, bodes well for the potential of this drug to treat CNS tumors. In orthotopic models, i.v. administration leads to greater tumor tissue accumulation than oral dosing, leading to greater bioavailability. |
激酶实验 | MiaPaca2 and BxPC-3 cells are treated with CBL0137 hydrochloride for 4 or 24 h. Cells are harvested in 1× Cell Culture Lysis Reagent containing protease and phosphatase inhibitors. Lysates 5 to 20 μg are separated on SDS-PAGE gels and transferred to PVDF membranes. Blots are probed with antibodies specific for SSRP1, SPT16, RRM1, and RRM2. |
细胞实验 | Effects of CBLC137 (2 μM for 24 hours) on cell cycle in tumor (HT1080, RCC45, MiaPaca) and normal cells (Wi38, NKE-hTERT) are examined using FACS analysis of propidium iodide-stained cells. |
动物实验 | Animal Models: xenograft mouse models of cancer. Formulation: water. Dosages: 30 mg/kg. Administration: p.o. |
别名 | CBL0137, CBLC137, Curaxin 137, CBL-C137 hydrochloride, Curaxin-137 hydrochloride |
分子量 | 372.88 |
分子式 | C21H25ClN2O2 |
CAS No. | 1197397-89-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: 25 mg/mL (67.05 mM), Sonification is recommended
DMSO: 36 mg/mL (96.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 2.6818 mL | 13.4091 mL | 26.8183 mL | 67.0457 mL |
5 mM | 0.5364 mL | 2.6818 mL | 5.3637 mL | 13.4091 mL | |
10 mM | 0.2682 mL | 1.3409 mL | 2.6818 mL | 6.7046 mL | |
20 mM | 0.1341 mL | 0.6705 mL | 1.3409 mL | 3.3523 mL | |
50 mM | 0.0536 mL | 0.2682 mL | 0.5364 mL | 1.3409 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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