PARP/VEGFR3-IN-1

PARP/VEGFR3-IN-1 (Compound 18) is a dual PARP-VEGFR3 target inhibitor. Its IC50 values for PARP1, PARP2, and VEGFR3 are 0.0763, 0.0366, and 4.25 nM respectively. PARP/VEGFR3-IN-1 has no inhibitory effect on VEGFR1/2 and shows subtype selectivity. PARP/VEGFR3-IN-1 exhibits significant anti-proliferative activity in various cancer cells (leukemia, lung cancer, and triple-negative breast cancer) . PARP/VEGFR3-IN-1 induces DNA damage and cell cycle arrest. PARP/VEGFR3-IN-1 triggers various forms of cell death by inducing apoptosis and autophagy. PARP/VEGFR3-IN-1 can be formulated into nanodelivery systems, significantly enhancing tumor targeting and therapeutic window[1].

Product Specifications

Target

Apoptosis; Autophagy; DNA/RNA Synthesis; PARP; VEGFR

Related Pathways

Apoptosis; Autophagy; Cell Cycle/DNA Damage; Epigenetics; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

COC1=CC=C(C2=NC=NC3=C2C=C(OC)C(OCCCN4C=C(CNC(C5=CC(CC6=NNC(C7=C6C=CC=C7)=O)=CC=C5F)=O)N=N4)=C3)C=C1

Molecular Formula

C38H33FN8O5

Molecular Weight

700.72

References & Citations

[1]Rana M, et al. Olaparib-Cediranib Hybrid as Dual PARP-VEGFR3 Inhibitor Elicits Antitumor Efficacy: Rational Design, Synthesis, Biological Evaluation and Construction of a Charge Convertible pH Responsive Nanoformulation. Bioorg Chem. 2025 Oct;165:109035.