S80118
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- 公司名稱 上海源葉生物科技有限公司
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- 產(chǎn)品描述： CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively
- 靶點(diǎn)： IC50: 54 nM (rRNA synthesis, MIA PaCa-2 cells), 113 nM (rRNA synthesis, A375 cells), 142 nM (rRNA synthesis, HCT-116 cells)
- 體內(nèi)研究： CX-5461 displays antitumor activity against human solid tumors in murine xenograft models. CX-5461 (50 mg/kg, p.o.) shows significant MIA PaCa-2 growth inhibition with TGI equal to 69% on day 31 and 79% TGI on A375 on day 32. CX-5461 (50 mg/kg, p.o.) inhibits the Eμ-Myc tumor cells with 84% repression in Pol I transcription at 1 hr posttreatment in C57BL/6 mice. CX-5461 also induces a rapid reduction in tumor burden in the lymph nodes and a concomitant reduction of spleen size to within the normal range
- 參考文獻(xiàn)：
1. Drygin D et al. Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth. Cancer Res. 2011 Feb 15;71(4):1418-30. 2. Bywater MJ, et al. Inhibition of RNA Polymerase I as a Therapeutic Strategy to Promote Cancer-Specific Activation of p53. Cancer Cell. 2012 Jul 10;22(1):51-65.
- 溶解度： 50 mM sodium phosphate (pH 3.5) : 10 mg/mL (19.47 mM; Need ultrasonic) DMSO : < 1 mg l (ultrasonic;warming;heat to 60°c) (insoluble or slightly soluble)="">
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 1.947 ml 9.735 ml 19.47 ml 5 mM 0.389 ml 1.947 ml 3.894 ml 10 mM 0.195 ml 0.974 ml 1.947 ml 50 mM 0.039 ml 0.195 ml 0.389 ml
- 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的性，僅供客戶參考交流研究之用。
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