产品
编 号：F754468
分子式：C26H24N2O6
分子量：460.48
分子式：C26H24N2O6
分子量：460.48
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2665734-13-2
产品详情
生物活性：
PD-1/PD-L1-IN-29 (S4-1) is a potent PD-1/PD-L1 inhibitor with an IC50 value of 6.1 nM. PD-1/PD-L1-IN-29 binds PD-L1 and disrupts PD-1/PD-L1 interactions, induces PD-L1 dimerization and internalization, improves its localization to the endoplasmic reticulum, and promotes PD-L1 entry into the endoplasmic reticulum. PD-1/PD-L1-IN-29 has anticancer activity.
体内研究：
PD-1/PD-L1-IN-29(S4-1)(10 or 25 mg/kg, i.p., 12 days) significantly inhibits tumour growth in the MC38 colorectal tumour mouse model, as observed in both the low and high dose groups (10 and 25 mg/kg), with inhibition rates of 65.9% and 88.8% respectively.The pharmacokinetic parameters of PD-1/PD-L1-IN-29(S4-1) in mice Parametersiv (5 mg/kg)po (50 mg/kg)T1/2 (h)9.784.77Tmax (h)0.080.92Cmax (ng/mL)6290260.67AUC0-t (h*ng/mL)3466.58/td>808.04AUC0-∞ (h*ng/mL)3566.62830.34CL (mL/h/kg)1404.22-
体外研究：
PD-1/PD-L1-IN-29(S4-1) (10 or 20 μM, 48 h) can increase the cytotoxicity of PBMCs against A375 tumor cells by blocking PD-1/PD-L1 interaction and restoring the activation state of PBMCs, with little direct killing effect on tumor cells.
PD-1/PD-L1-IN-29 (S4-1) is a potent PD-1/PD-L1 inhibitor with an IC50 value of 6.1 nM. PD-1/PD-L1-IN-29 binds PD-L1 and disrupts PD-1/PD-L1 interactions, induces PD-L1 dimerization and internalization, improves its localization to the endoplasmic reticulum, and promotes PD-L1 entry into the endoplasmic reticulum. PD-1/PD-L1-IN-29 has anticancer activity.
体内研究：
PD-1/PD-L1-IN-29(S4-1)(10 or 25 mg/kg, i.p., 12 days) significantly inhibits tumour growth in the MC38 colorectal tumour mouse model, as observed in both the low and high dose groups (10 and 25 mg/kg), with inhibition rates of 65.9% and 88.8% respectively.The pharmacokinetic parameters of PD-1/PD-L1-IN-29(S4-1) in mice Parametersiv (5 mg/kg)po (50 mg/kg)T1/2 (h)9.784.77Tmax (h)0.080.92Cmax (ng/mL)6290260.67AUC0-t (h*ng/mL)3466.58/td>808.04AUC0-∞ (h*ng/mL)3566.62830.34CL (mL/h/kg)1404.22-
体外研究：
PD-1/PD-L1-IN-29(S4-1) (10 or 20 μM, 48 h) can increase the cytotoxicity of PBMCs against A375 tumor cells by blocking PD-1/PD-L1 interaction and restoring the activation state of PBMCs, with little direct killing effect on tumor cells.
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