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CBL0137 hydrochloride

CAS No. 1197397-89-9

CBL0137 hydrochloride ( CBL0137 | CBL-0137 | CBL 0137 | Curaxin 137 )

产品货号. M17184 CAS No. 1197397-89-9

在基于细胞的 p53 和 NF-kB 报告基因检测中,CBL0137 分别激活 p53 并抑制 NF-kB(EC50:0.37/0.47 μM)。它还抑制组蛋白伴侣 FACT。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥494 有现货
5MG ¥1061 有现货
10MG ¥1839 有现货
25MG ¥3977 有现货
50MG ¥5800 有现货
100MG ¥7655 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    CBL0137 hydrochloride
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    在基于细胞的 p53 和 NF-kB 报告基因检测中,CBL0137 分别激活 p53 并抑制 NF-kB(EC50:0.37/0.47 μM)。它还抑制组蛋白伴侣 FACT。
  • 产品描述
    CBL0137 (CBL-0137) activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).(In Vitro):Treatment with CBL0137 hydrochloride leads to complete absence of living cells at concentrations above 2.5 μM. CBL0137 hydrochloride causes a greater reduction in the number of colonies formed of not only MiaPaCa-2 cells when combines with gemcitabine, but also gemcitabine-resistant PANC-1 cells. Treatment of human pancreatic cancer cells with CBL0137 hydrochloride results in a dose dependent reduction of protein and mRNA levels of RRM1 and RRM2. (In Vivo):The CBL0137 hydrochloride monotherapy group and the CBL0137 hydrochloride-gemcitabine combination group samples show large necrotic fields, numerous apoptotic bodies and loss of tumor cells. Sub-optimal doses of 50 to 60 mg/kg CBL0137 hydrochloride causes similar enhancement of gemcitabine antitumor activity as that produced by the maximum tolerated dose (MTD) of 90 mg/kg as indicated by the lack of statistically significant differences among the combination groups. CBL0137 hydrochloride inhibits FACT function through depletion of the pool of active FACT involved in transcription elongation. CBL0137 hydrochloride, given by oral gavage at a nontoxic dose of 30 mg/kg per day on a 5 days on/2 days off schedule, suppresses tumor growth in xenografts of colon (DLD-1), renal cell carcinoma (Caki-1), and melanoma (Mel-7) tumor cell lines and transplanted surgical samples from patients with pancreatic ductal adenocarcinoma.
  • 体外实验
    Treatment with CBL0137 hydrochloride leads to complete absence of living cells at concentrations above 2.5 μM. CBL0137 hydrochloride causes a greater reduction in the number of colonies formed of not only MiaPaCa-2 cells when combines with gemcitabine, but also gemcitabine-resistant PANC-1 cells. Treatment of human pancreatic cancer cells with CBL0137 hydrochloride results in a dose dependent reduction of protein and mRNA levels of RRM1 and RRM2.
  • 体内实验
    The CBL0137 hydrochloride monotherapy group and the CBL0137 hydrochloride-gemcitabine combination group samples show large necrotic fields, numerous apoptotic bodies and loss of tumor cells. Sub-optimal doses of 50 to 60 mg/kg CBL0137 hydrochloride causes similar enhancement of gemcitabine antitumor activity as that produced by the maximum tolerated dose (MTD) of 90 mg/kg as indicated by the lack of statistically significant differences among the combination groups. CBL0137 hydrochloride inhibits FACT function through depletion of the pool of active FACT involved in transcription elongation. CBL0137 hydrochloride, given by oral gavage at a nontoxic dose of 30 mg/kg per day on a 5 days on/2 days off schedule, suppresses tumor growth in xenografts of colon (DLD-1), renal cell carcinoma (Caki-1), and melanoma (Mel-7) tumor cell lines and transplanted surgical samples from patients with pancreatic ductal adenocarcinoma.
  • 同义词
    CBL0137 | CBL-0137 | CBL 0137 | Curaxin 137
  • 通路
    Apoptosis
  • 靶点
    IL Receptor
  • 受体
    FACT|p53|NF-κB
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    1197397-89-9
  • 分子量
    372.88
  • 分子式
    C21H25ClN2O2
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO : 30 mg/mL. 80.45 mM; H2O : 15.2 mg/mL. 40.76 mM
  • SMILES
    CC(C)NCCN1C2=C(C=C(C=C2)C(=O)C)C3=C1C=CC(=C3)C(=O)C.Cl
  • 化学全称
    1,1'-(9-(2-((1-Methylethyl)imino)ethyl)-9H-carbazole-3,6-diyl)bisethanone, hydrochloride (1:1)

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

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.
产品手册
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