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S82313

Triazolo-pyramidine derivative

源叶(MedMol) 99%
  • 英文名:
  • Triazolo-pyramidine derivative
  • 别名:
  • (S)-7-(5-methylfuran-2-yl)-3-(6-[tetrahydrofuran-3-yl]oxymethylpyrid-2-ylmethyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine
  • CAS号:
  • 1202402-40-1
  • 分子式:
  • C20H21N7O3
  • 分子量:
  • 407.42584
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S82313-1mg 99% ¥390.00元 >10 - - - EA 加入购物车
源叶(MedMol) S82313-5mg 99% ¥900.00元 >10 - - - EA 加入购物车
源叶(MedMol) S82313-10mg 99% ¥1500.00元 >10 - - - EA 加入购物车
源叶(MedMol) S82313-50mg 99% ¥4000.00元 >10 - - - EA 加入购物车
源叶(MedMol) S82313-100mg 99% ¥6000.00元 10 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Ciforadenant (CPI-444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses
  • 靶点: Adenosine A2A receptor
  • 体外研究:
    Ciforadenant is a potent, oral, selective A2AR antagonist. CD8+ T cell depletion abrogates the efficacy of Ciforadenant treatment as a single agent as well as in combination with anti-PD-L1, demonstrating a role for CD8+ T cells in mediating primary and secondary immune responses. Anti-tumor efficacy of Ciforadenant±anti-PD-L1 is associated with increased CD8+ cell infiltration and activation in MC38 tumor tissues, and a corresponding rise in PD-1 expression on CD8+ T cells in the spleen. Additionally, levels of immune checkpoints are modulated by treatment with Ciforadenant, including GITR, OX40, and LAG3 on tumor infiltrating lymphocytes and circulating T cells, suggesting a broad role for adenosine mediated immunosuppression
  • 体内研究:
    Daily treatment of the syngeneic mouse model MC38 with Ciforadenant (1, 10, 100 mg/kg) leads to dose-dependent inhibition of tumor growth, leading to tumor elimination in ~30% of treated mice. Combining Ciforadenant (100 mg/kg, qd, 14 days) with anti-PD-L1 (200 μg, 3qw, 4 doses) treatment in MC38 models synergistically inhibits tumor growth and eliminates tumors in 90% of treated mice. When cured mice are later re-challenged with MC38 cells, tumor growth is rejected in 100% of challenged mice, indicating that Ciforadenant induces systemic anti-tumor immune memory
  • 参考文献:
    1. Stephen Willingham, et al. Abstract PR04: CPI-444: A potent and selective inhibitor of A2AR induces antitumor responses alone and in combination with anti-PD-L1 in preclinical and clinical studies.Cancer Immunoly Research. September 25-28, 2016.
  • 溶解性: soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.454 ml 12.272 ml 24.544 ml
    5 mM 0.491 ml 2.454 ml 4.909 ml
    10 mM 0.245 ml 1.227 ml 2.454 ml
    50 mM 0.049 ml 0.245 ml 0.491 ml
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