VEGFR/PD-L1-IN-1 

VEGFR/PD-L1-IN-1 is a VEGFR2 and PD-L1 inhibitor, with IC₅₀ values of 0.383 μM and 134.407 pg/mL against VEGFR2 and PD-L1, respectively. VEGFR/PD-L1-IN-1 enhances the secretion of INF-γ, induces G0/G1 cell cycle arrest in cancer cells, and triggers cancer cell apoptosis. VEGFR/PD-L1-IN-1 upregulates the expression of BAX and Caspase-3, and downregulates the expression of Bcl-2. VEGFR/PD-L1-IN-1 can be used in research related to hepatocellular carcinoma, prostate cancer, and colorectal cancer^[1].

VEGFR/PD-L1-IN-1 (Compound 8g) potently inhibits the growth of HepG2, PC-3 and HCT-116 cancer cells with IC₅₀ values of 3.93 μM, 9.56 μM and 6.30 μM, respectively, while exhibits low cytotoxicity against normal WI-38 cells^[1].
VEGFR/PD-L1-IN-1 induces G₀/G₁ cell cycle arrest in HepG2 cells, thereby reducing cell progression to the S and G₂/M phases^[1].
VEGFR/PD-L1-IN-1 induces significant apoptosis and necrosis in HepG2 cells^[1].
VEGFR/PD-L1-IN-1 promotes INF-γ secretion and activates the intrinsic apoptotic pathway in HepG2 cells by upregulating the expression of BAX and Caspase-3 and downregulating the expression of Bcl-2^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

418.41

C₂₁H₁₈N₆O₄

2675913-94-5

O=C(N/N=C/C1=CC=C(O)C(OC)=C1)CN(C=NC2=C3C=NN2C4=CC=CC=C4)C3=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Hassoub EMM, et al. Design, synthesis, and mechanistic study of bispecific small molecules-based phenyl pyrazolopyrimidinone scaffold as dual-targeting VEGFR and PD-L1 immune checkpoint in hepatocellular carcinoma. Bioorg Chem. 2026;175:109789.