货号	规格	价格	上海	北京	珠海	重庆	武汉
S82313-1mg买3赠1	≥99%	￥80.00 S82313-1mg ￥80.00 现货（买3赠1）	1000 >10	-	-	-	-
S82313-5mg买3赠1	≥99%	￥150.00 S82313-5mg ￥150.00 现货（买3赠1）	200 >10	-	-	-	-
S82313-10mg买3赠1	≥99%	￥260.00 S82313-10mg ￥260.00 现货（买3赠1）	100 >10	-	-	-	-
S82313-50mg买3赠1	≥99%	￥750.00 S82313-50mg ￥750.00 现货（买3赠1）	20 >10	-	-	-	-
S82313-100mg买3赠1	≥99%	￥1280.00 S82313-100mg ￥1280.00 现货（买3赠1）	10 10	-	-	-	-

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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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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Triazolo-pyramidine derivative