CX-5461は一種のrRNA synthesis阻害剤ですが、Pol Iが駆動したrRNA転写を選択制的に抑制して、HCT-116、A375とMIA PaCa-2の細胞にIC50値が142nMになって、Pol IIに作用を表さなくて、rRNA転写を抑制する選択性はDNA複製とタンパク質翻訳を抑制する選択性より250倍-300倍が高くなります。

サイズ 価格 在庫  
JPY 38876.76 あり
JPY 53275.56 あり
JPY 139668.35 あり


  • Representative western blot evaluation and densitormetric analysis of p53 expression in control and CX-5461 (CX)-treated HCT116, HepG2, MCF7 and LoVo cells. Cells were exposed to 1 μM CX-5461 for 12 h.

    Oncogene, 2015, 10.1038/onc.2015.147. CX-5461 purchased from Selleck.

    The specific Pol I inhibitor CX-5461 causes nucleolar disruption, blocks LTP maintenance and Fsk-induced synthesis of new rRNA. DAPI staining (blue; A, B,C) shows the area of the nucleus. Nomarski images (grey; G, H,I) show the area of the nuclei and nucleoli (arrowheads). Application of Pol I specific inhibitor CX-5461 (200 nM) causes nucleolar disruption as indicated by the distribution of fibrillarin (green); compare A, D to B, E and C, F.

    PLoS One 2014 9(8), e104364. CX-5461 purchased from Selleck.

  • (B) After CX-5461 treatment at different concentrations for 72 hours, whole cell lysates from OS cells were subjected to Western blot analysis using LC3B-II and actin antibodies. (C) The cells were incubated with 2 mM CX-5461 with or without 2.5 mM 3-MA for 72 hours. The percentage of cell death was determined by CellTiter-Glo™ Luminescent Cell Viability Assay. The data represent the mean of three separate experiments performed in triplicate; bars represent SD. *P<0.05; **P<0.01. +, treatment; −, no treatment. Abbreviations: 3-MA, 3-methyladenine; OS, osteosarcoma; SD, standard deviation.

    Onco Targets Ther, 2016, 9:5985-5997.. CX-5461 purchased from Selleck.


DNA/RNA Synthesis阻害剤の選択性比較


製品説明 CX-5461は一種のrRNA synthesis阻害剤ですが、Pol Iが駆動したrRNA転写を選択制的に抑制して、HCT-116、A375とMIA PaCa-2の細胞にIC50値が142nMになって、Pol IIに作用を表さなくて、rRNA転写を抑制する選択性はDNA複製とタンパク質翻訳を抑制する選択性より250倍-300倍が高くなります。
Pol I-driven transcription of rRNA [1]
(HCT-116, A375, MIA PaCa-2 cells)
142 nM

CX-5461 is found to selectively inhibit rRNA synthesis (Pol I IC50=142 nM; Pol II IC50 > 25 μM; selectivity ~200-fold) in the HCT-116 cells. Selective inhibition of rRNA synthesis by CX-5461 is confirmed in two other human solid tumor cell lines; melanoma A375 (Pol I IC50 = 113 nM; Pol II IC50 > 25 μM) and pancreatic carcinoma MIA PaCa-2 (Pol I IC50=54 nM; Pol II IC50 ~25 mM). CX-5461 possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation. CX-5461 exhibits broad antiproliferative potency in a panel of cancer cell lines in human cancer cell lines, but has minimal effect on viability of nontransformed human cells. The median EC50 across all tested cell lines is 147 nM, yet all normal cell lines have EC50 values of approximately 5, 000 nM. Evaluation of the antiproliferative dose response for HCT-116, A375, and MIA PaCa-2 cell lines yield EC50 values of 167, 58, and 74 nM. CX-5461 induces autophagy and senescence in solid tumor cancer cells, rather than apoptosis, through a p53-independent process. [1]

体内試験 CX-5461 is orally bioavailable and demonstrates in vivo antitumor activity against human solid tumors in murine xenograft models. CX-5461 demonstrates significant MIA PaCa-2 TGI with TGI equal to 69% on day 31, comparable to that of gemcitabine (63% TGI). Gemcitabine is a positive control which is administered intraperitoneally once every 3 days at 120 mg/kg. Likewise, CX- 5461 demonstrates significant A375 TGI with TGI equal to 79% on day 32. [1]


+ 展開

Pol I and Pol II Transcription Assay:

Two short-lived RNA transcripts (half-lives ~20-30 minutes), one produced by Pol I and another by Pol II, are quantitated by qRT-PCR as a measure of CX-5461-related effects on transcription. The 45S pre-rRNA served as the Pol I transcript and the mRNA for the protooncogene c-myc served as the comparator Pol II transcript. Both Pol I and Pol II transcription are known to be affected by general cellular stress. To minimize the potential effects of such stress, cells are exposed to test agents for only a short period of time (2 hours). This is sufficient time for these transcripts to be reduced by greater than 90% if CX-5461 affects their synthesis.
細胞試験: [1]
+ 展開
  • 細胞株: panel of cancer and normal cell lines
  • 濃度: 0-2 μM
  • 反応時間: 96 hours
  • 実験の流れ: Cells are plated on 96-well plates and treated the next day with dose response of CX-5461 for 96 hours. Cell viability is determined using Alamar Blue and CyQUANT assays
+ 展開
  • 動物モデル: 5 × 106 MIA Paca-2 and A375 cancer cells are subcutaneously inoculated in the right flank of 5- to 6- week-old female athymic mice
  • 製剤: CX-5461 is dissolved in 50 mM NaH2PO4 (pH 4.5).
  • 投薬量: 50 mg/kg
  • 投与方法: CX-5461 is administered orally once daily or every 3 days.

溶解度 (25°C)

体外 DMF 3 mg/mL (5.84 mM) warming
DMSO 0.02 mg/mL (0.03 mM)
Water Insoluble

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。


分子量 513.61


CAS No. 1138549-36-6
in solvent
別名 N/A





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


マス 濃度 ボリューム 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02719977 Recruiting Cancer Canadian Cancer Trials Group|Senhwa Biosciences, Inc.|Stand Up To Cancer May 2016 Phase 1|Phase 2



Handling Instructions


  • * 必須


  • 問題1:

    I want to make it for further in vivo treatment. I

  • 回答:

    The solubility of this compound is poor in common vehicles. It can be dissolved in DMF at 3 mg/ml with warming.

DNA/RNA Synthesis信号経路図

相関DNA/RNA Synthesis製品

Tags: CX-5461を買う | CX-5461 ic50 | CX-5461供給者 | CX-5461を購入する | CX-5461費用 | CX-5461生産者 | オーダーCX-5461 | CX-5461化学構造 | CX-5461分子量 | CX-5461代理店
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID