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  • EBI-2511
    EBI-2511的可视化放大

    EBI-2511

    EBI-2511是具有口服活性的、EZH2的有效抑制剂,其在Pfeffiera细胞中的IC50值为6nM。

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    EBI-2511的二维码
    • 库存: 现货
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    • 5mg
      ¥1937.00
      1550.00
      - +
    • 10mg
      ¥3012.00
      2410.00
      - +
    • 25mg
      ¥6200.00
      4960.00
      - +
    • 50mg
      ¥9087.00
      7270.00
      - +
    • 100mg
      ¥14287.00
      11430.00
      - +
    已选 0 0
    金额: ¥0.00
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    • 货号: ajce50682
    • CAS: 2098546-05-3
    • 别名:
    • 分子式: C34H48N4O4
    • 分子量: 576.77
    • 纯度: >98%
    • 溶解度: DMSO : 5 mg/mL (8.67 mM)
    • 储存: Store at -20°C
    • 库存: 现货

    Background

    EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.


    EBI-2511 (Compound 34) significantly reduces cellular H3K27me3 levels in a dose-dependent manner with an approximate IC50 of 8 nM, which is 3-fold more potent than EPZ-6438. In addition to Pfeffier cell line, EBI-2511 was shown active with IC50 value of 55 nM against WSU-DLCL2[1].


    EBI-2511 displays a dose-dependent inhibition on the tumor growth, resulting in 28% (10mg/kg), 83% (30mg/kg), and 97% (100mg/kg) reduction in tumor size. At the same dosage level, EBI-2511 shows a superior anti-tumor efficacy to EPZ-6438 (P<0.01). It is noteworthy that no significant changes in body weights of all treatment groups are observed[1].


    [1]. Lu B, et al. Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma. ACS Med Chem Lett. 2018 Jan 29;9(2):98-102.

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