PD-1/PD-L1-IN-10 (compound B2) is an orally active PD-1/PD-L1 inhibitor ( IC 50 of 2.7 nM) with potent anticancer efficacy
In Vitro
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. PD-1/PD-L1-IN-10 (compound B2) does not affect cell viability of LLC cells and lymph node T-cells. PD-1/PD-L1-IN-10 (compound B2, 0-100 nM) stabilizes the PD-L1 protein in mouse Lewis lung carcinoma (LLC) cells. In particular, 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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. . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: LLC tumor-bearing mice . Dosage: 2, 5 mg/kg. Administration: i.g., qd., for 21 days Result: Significantly suppressed the growth of the tumor in a dose-dependent manner compared with the vehicle group.