S82313 |
Triazolo-pyramidine derivative |
源叶(MedMol) | 99% |
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- 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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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)