PD-1/PD-L1-IN-10 |
| رقم الكتالوجGC62125 |
PD-1 / PD-L1-IN-10 (المركب B2) هو مثبط PD-1 / PD-L1 نشط عن طريق الفم (IC50 من 2.7 نانومتر) مع فعالية قوية مضادة للسرطان
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2487550-41-2
Sample solution is provided at 25 µL, 10mM.
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PD-1/PD-L1-IN-10 (compound B2) is an orally active PD-1/PD-L1 inhibitor (IC50 of 2.7 nM) with potent anticancer efficacy[1].
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. 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[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].
[1]. Yiqiang OuYang, et al. Design, Synthesis, and Evaluation of o-(Biphenyl-3-ylmethoxy)nitrophenyl Derivatives as PD-1/PD-L1 Inhibitors with Potent Anticancer Efficacy In Vivo. J Med Chem. 2021 May 26.
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