PD-1/PD-L1-IN-10 是一种口服有效的PD-1/PD-L1抑制剂 (IC50of 2.7 nM)，显示出抗肿瘤活性。

PD-1/PD-L1-IN-10 is an orally active PD-1/PD-L1 inhibitor (IC50 of 2.7 nM) with potent anticancer efficacy.

PD-1/PD-L1-IN-10 (compound B2) significantly promotes interferongamma secretion in a dose-dependent manner in vitro even at the low concentration of 1 nM[1]. PD-1/PD-L1-IN-10 (compound B2) does not affect cell viability of LLC cells and lymph node T-cells[1]. PD-1/PD-L1-IN-10 (compound B2, 0-100 nM) stabilizes the PD-L1 protein in mouse Lewis lung carcinoma (LLC) cells. Especially, PD-1/PD-L1-IN-10 (compound B2) maintains the PD-L1 stability in a dose-dependent manner at 58 °C.Suggesting that PD-1/PD-L1-IN-10 (compound B2) could enter LLC cells and then directly binds to the PD-L1 protein[1].

PD-1/PD-L1-IN-10 (compound B2, 5 mg/kg, intragastric gavage) exhibits potent in vivo anticancer efficacy in an LLC-bearing allograft mouse model. PD-1/PD-L1-IN-10 (compound B2) effectively blocks tumor cell proliferation and induces apoptosis in LLC tumor tissues.[1].

2487550-41-2

C33H31N3O7

581.62

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