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编 号：F756908
分子式：C27H25N5O2
分子量：451.52
分子式：C27H25N5O2
分子量：451.52
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CAS No: 2922920-71-4
产品详情
生物活性：
A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2).
体内研究：
A2AR-antagonist-1（100 mg/kg；口服；每天一次，持续 23 天）在携带结肠癌 MC38 细胞的 C57BL/6 小鼠体内表现出优异的抗肿瘤活性。在小鼠中的药代动力学分析RouteDose (mg/kg)Cmax (ng/mL)AUC0-last (ng·h/mL)AUC0-t (ng·h/mL)t1/2 (h)F (%)
i.v.22584557755650.93/
p.o.10882324008240032.3586.1
Animal Model:MC38 xenograft model in mouse
Dosage:100 mg/kg
Administration:PO; once daily for 23 days
Result:Promoted CD8+ T cell accumulation.Enhanced antitumor immunity, promoted tumor regression.Had insignificant effect on body weight of the mice.
体外研究：
A2AR-antagonist-1（0.001-10 μM；30 分钟）降低 HEK293-A2AR 细胞中 NECA 诱导的磷酸化 ERK 水平。A2AR-antagonist-1（0.1-10 μM；5 小时）抑制 NECA 诱导的免疫分子表达并增加 Jurkat T 细胞（人永生化 T 淋巴细胞系） 中的效应分子表达。A2AR-antagonist-1（0.1-10 μM; 48 h）恢复 OT-I 小鼠脾细胞 (OT-I CTL) 对 MC38-OVA 细胞的细胞毒功能损伤，增强体外 T 细胞的活化和效应功能。
A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2).
体内研究：
A2AR-antagonist-1（100 mg/kg；口服；每天一次，持续 23 天）在携带结肠癌 MC38 细胞的 C57BL/6 小鼠体内表现出优异的抗肿瘤活性。在小鼠中的药代动力学分析RouteDose (mg/kg)Cmax (ng/mL)AUC0-last (ng·h/mL)AUC0-t (ng·h/mL)t1/2 (h)F (%)
i.v.22584557755650.93/
p.o.10882324008240032.3586.1
Animal Model:MC38 xenograft model in mouse
Dosage:100 mg/kg
Administration:PO; once daily for 23 days
Result:Promoted CD8+ T cell accumulation.Enhanced antitumor immunity, promoted tumor regression.Had insignificant effect on body weight of the mice.
体外研究：
A2AR-antagonist-1（0.001-10 μM；30 分钟）降低 HEK293-A2AR 细胞中 NECA 诱导的磷酸化 ERK 水平。A2AR-antagonist-1（0.1-10 μM；5 小时）抑制 NECA 诱导的免疫分子表达并增加 Jurkat T 细胞（人永生化 T 淋巴细胞系） 中的效应分子表达。A2AR-antagonist-1（0.1-10 μM; 48 h）恢复 OT-I 小鼠脾细胞 (OT-I CTL) 对 MC38-OVA 细胞的细胞毒功能损伤，增强体外 T 细胞的活化和效应功能。
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