產(chǎn)品介紹：
CPI-444 是一種有效的選擇性 A2A 受體 (A2AR) 拮抗劑，誘導(dǎo)抗腫瘤反應(yīng)。
靶點：Adenosine A2A receptor[1]
體外作用：
CPI-444 is a potent, oral, selective A2AR antagonist. CD8+ T cell depletion abrogates the efficacy of CPI-444 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 CPI-444±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 CPI-444, including GITR, OX40, and LAG3 on tumor infiltrating lymphocytes and circulating T cells, suggesting a broad role for adenosine mediated immunosuppression[1].
體內(nèi)作用：
Daily treatment of the syngeneic mouse model MC38 with CPI-444 (1, 10, 100 mg/kg) leads to dose-dependent inhibition of tumor growth, leading to tumor elimination in ~30% of treated mice. Combining CPI-444 (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 CPI-444 induces systemic anti-tumor immune memory[1].
溶解方案參考：
請根據(jù)您的實驗動物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮Ｒ韵氯芙夥桨付颊埾劝凑?In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
??? 1.
??? 請依序添加每種溶劑： 10% DMSO??? 40% PEG300??? 5% Tween-80??? 45% saline
??? Solubility: ≥ 2.25 mg/mL (5.52 mM); Clear solution
??? 2.
??? 請依序添加每種溶劑： 10% DMSO??? 90% (20% SBE-β-CD in saline)
??? Solubility: ≥ 2.25 mg/mL (5.52 mM); Clear solution
*以上所有助溶劑都可在 MCE 網(wǎng)站選購。
參考文獻(xiàn)：
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