Drug intelligence / Profile preview

Lanzhou Univ. VEGFR-2 compound P7

Development stage
Preclinical
Lead developer
Lanzhou University
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules
01

Overview

Lanzhou Univ. VEGFR-2 compound P7: sourced facts only. name: "Among them, P7 exhibited preferable antitumor activity against HGC-27 cells and less toxic to human normal HUVEC, HEK293T and GES-1 cells in vitro, as well as the potent degradation activity of VEGFR-2 protein in HGC-27 cells (DC50: 0.084 ± 0.04 μM, Dmax: 73.7%) and HUVEC cells (DC50: 0.51 ± 0.10 μM, Dmax: 76.6%)." [PMID:36242985]; target: "Among them, P7 exhibited preferable antitumor activity against HGC-27 cells and less toxic to human normal HUVEC, HEK293T and GES-1 cells in vitro, as well as the potent degradation activity of VEGFR-2 protein in HGC-27 cells (DC50: 0.084 ± 0.04 μM, Dmax: 73.7%) and HUVEC cells (DC50: 0.51 ± 0.10 μM, Dmax: 76.6%)." [PMID:36242985]; developer: "School of Pharmacy & Collaborative Innovation Center for Northwestern Chinese Medicine, Lanzhou University, Lanzhou, 730000, China." [PMID:36242985]; modality: "All the results demonstrated that P7 could be as a promising VEGFR-2-PROTAC degrader for gastric cancer therapy." [PMID:36242985]; stage: "Moreover, P7 inhibited the colony formation, migration and invasion of HGC-27 cells in a time- and dose-dependent manner, and meanwhile induced G2/M phase cycle arrest and apoptosis." [PMID:36242985]

02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)

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