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CBL0137 hydrochloride

CBL0137 hydrochloride

产品编号 T4361   CAS 1197397-89-9
别名: CBL0137, CBLC137, Curaxin 137, CBL-C137 hydrochloride, Curaxin-137 hydrochloride

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。

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CBL0137 hydrochloride Chemical Structure
CBL0137 hydrochloride, CAS 1197397-89-9
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
其他形式的 CBL0137 hydrochloride:
产品目录号及名称: CBL0137 hydrochloride (T4361)
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纯度: 98.59%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

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)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Gasparian AV,etal.Curaxins: anticancer compounds that simultaneously suppress NF-κB and activate p53 by targeting FACT.Sci Transl Med. 2011 Aug 10;3(95):95ra74. 2. Burkhart C,etal.Curaxin CBL20137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preClinicalal models of pancreatic cancer.Oncotarget. 2014 Nov 30;5(22):11038-53. 3. Barone TA,etal.Anticancer drug candidate CBL20137, which inhibits histone chaperone FACT, is efficacious in preClinicalal orthotopic models of temozolomide-responsive and -resistant glioblastoma.Neuro Oncol. 2017 Feb 1;19(2):186-196.
Ginsenoside Rs3 RITA p53-Mdm2 inhibitor 4 CP-31398 dihydrochloride IVHD-valtrate Indole-3-carbinol HBX 41108 Alphitolic acid

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 抗癌活性化合物库 抗乳腺癌化合物库 转录因子库 已知活性化合物库 泛素化化合物库 临床期小分子药物库 HIF-1化合物库 细胞凋亡化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
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技术支持

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。

Keywords

CBL0137 hydrochloride 1197397-89-9 Apoptosis NF-Κb Others NF-κB p53 Curaxin-137 Nuclear factor-κB CBL-C 137 Hydrochloride CBL0137 inhibit CBL0137 Hydrochloride Inhibitor CBL-0137 Hydrochloride Curaxin137 CBL-C137 CBLC137 CBL 0137 Nuclear factor-kappaB Curaxin 137 CBLC 137 MDM-2/p53 CBL-0137 CBL-C137 hydrochloride CBL-0137 hydrochloride Curaxin-137 Hydrochloride CBL-C-137 Hydrochloride CBL-C137 Hydrochloride CBLC-137 Curaxin-137 hydrochloride CBL 0137 Hydrochloride inhibitor

 

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