Bioactivity | 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[1]. |
Invitro | 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[1]. |
In Vivo | 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[1].The pharmacokinetic parameters of PD-1/PD-L1-IN-29(S4-1) in mice Parameters |
Name | PD-1/PD-L1-IN-29 |
CAS | 2665734-13-2 |
Formula | C26H24N2O6 |
Molar Mass | 460.48 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Chengliang Sun, et al. Novel Small-Molecule PD-L1 Inhibitor Induces PD-L1 Internalization and Optimizes the Immune Microenvironment. J Med Chem. 2022 Dec 29. |