产品
编 号：F741685
分子式：C22H24N2O2
分子量：348.44
分子式：C22H24N2O2
分子量：348.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 2628506-54-5
产品详情
生物活性：
PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model.
体内研究：
PD-1/PD-L1-IN-9 (化合物24) (40-80 mg/kg;口服; 每天一次，持续 2 周) 以剂量依赖的方式抑制肿瘤生长，并且不会导致小鼠体重减轻或死亡。PD-1/PD-L1-IN-9 (3 mg/kg; 静脉注射; 单次剂量) 在大鼠中的半衰期 T1/2=4.2 h、血浆清除率 Cl=11.5 L/h/kg，Cmax=1233 ng/mL。PD-1/PD-L1-IN-9 (25 mg/kg; 口服; 单次剂量) 在大鼠中表现出中等的口服生物利用度 (F= 22%)、半衰期 t1/2=6.4 h，Cmax=192 ng/mL。Animal Model:Male BALB/c mice (5-6 weeks) were inoculated CT26 cells
Dosage:40 mg/kg, 80 mg/kg
Administration:Oral gavage; once daily, for 2 weeks
Result:Significantly decreased the final tumor weight, with TGI values of 60 and 67% at the dose of 40 and 80 mg/kg, respectively.
Animal Model:Pharmacokinetic analysis in sprague-Dawley (SD) rats
Dosage:3 mg/kg and 25 mg/kg
Administration:Intravenous injection or oral gavage; single dose
Result:RouteDose (mg/kg)AUC(0-t) (ng·h/mL)Cmax (ng/mL)t1/2 (h)TmaxCl (L·h/kg)Vz (L/kg)F (%)
i.v.3430.512334.20.0311.578.6/
p.o.25787.41926.40.6928.8249.322
体外研究：
PD-1/PD-L1-IN-9 (compound 24) (46.9-1500 nM; 预处理 2 h) 剂量依赖性地激活外周血单核细胞 (PBMCs) 对 MDB-MB 231 细胞的抗肿瘤免疫，EC50 约为 100 nM。
PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model.
体内研究：
PD-1/PD-L1-IN-9 (化合物24) (40-80 mg/kg;口服; 每天一次，持续 2 周) 以剂量依赖的方式抑制肿瘤生长，并且不会导致小鼠体重减轻或死亡。PD-1/PD-L1-IN-9 (3 mg/kg; 静脉注射; 单次剂量) 在大鼠中的半衰期 T1/2=4.2 h、血浆清除率 Cl=11.5 L/h/kg，Cmax=1233 ng/mL。PD-1/PD-L1-IN-9 (25 mg/kg; 口服; 单次剂量) 在大鼠中表现出中等的口服生物利用度 (F= 22%)、半衰期 t1/2=6.4 h，Cmax=192 ng/mL。Animal Model:Male BALB/c mice (5-6 weeks) were inoculated CT26 cells
Dosage:40 mg/kg, 80 mg/kg
Administration:Oral gavage; once daily, for 2 weeks
Result:Significantly decreased the final tumor weight, with TGI values of 60 and 67% at the dose of 40 and 80 mg/kg, respectively.
Animal Model:Pharmacokinetic analysis in sprague-Dawley (SD) rats
Dosage:3 mg/kg and 25 mg/kg
Administration:Intravenous injection or oral gavage; single dose
Result:RouteDose (mg/kg)AUC(0-t) (ng·h/mL)Cmax (ng/mL)t1/2 (h)TmaxCl (L·h/kg)Vz (L/kg)F (%)
i.v.3430.512334.20.0311.578.6/
p.o.25787.41926.40.6928.8249.322
体外研究：
PD-1/PD-L1-IN-9 (compound 24) (46.9-1500 nM; 预处理 2 h) 剂量依赖性地激活外周血单核细胞 (PBMCs) 对 MDB-MB 231 细胞的抗肿瘤免疫，EC50 约为 100 nM。
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