VEGFR-2-IN-81 

VEGFR-2-IN-81 is a thiazole-based isoquinolin-1(2H)-one derivative and an VEGFR-2 inhibitor with IC₅₀ of 1.94 μM. VEGFR-2-IN-81 exhibits significant selective cytotoxicity against colorectal cancer cells (IC₅₀ = 7.75 μM). VEGFR-2-IN-81 exerts anti-colorectal cancer effects by inducing apoptosis, elevating intracellular ROS levels and reducing mitochondrial transmembrane potential. VEGFR-2-IN-81 can be used for the research of colorectal cancer, lung cancer, breast cancer, liver cancer^[1].

VEGFR-2-IN-81 (compound 3h) exhibits selective cytotoxicity against multiple cancer cell lines, with cytotoxic IC₅₀ values of 25.81 μM in MCF-7 cells, 7.75 μM in HCT-116 cells, 14.61 μM in A549 cells and 28.27 μM in HEPG-2 cells, and shows no obvious cytotoxicity (IC₅₀ > 35 μM) against normal HEK-293 cells^[1].
VEGFR-2-IN-81 inhibits purified VEGFR-2 kinase activity with an IC₅₀ of 1.94 μM^[1].
VEGFR-2-IN-81 (2-15 μM; 24 h) induces apoptotic morphological changes and apoptosis in HCT-116 human colon cancer cells in a concentration-dependent manner^[1].
VEGFR-2-IN-81 (2-15 μM; 24 h) increases intracellular ROS levels in HCT-116 human colon cancer cells in vitro in a concentration-dependent manner^[1].
VEGFR-2-IN-81 (2-15 μM; 24 h) disrupts mitochondrial membrane potential in HCT-116 human colon cancer cells in vitro in a concentration-dependent manner^[1].

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

470.34

C₂₁H₁₆BrN₃O₃S

O=C1N(C2=NC(C3=CC=C(Br)C=C3)=CS2)C(N)=C(C(OCC)=O)C4=CC=CC=C41

Room temperature in continental US; may vary elsewhere.

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

• [1]. Gupta S,et al. Copper(II)-catalysed one-pot synthesis of thiazole/benzothiazole-based isoquinolin-1(2H)-ones as potential cytotoxic and VEGFR-2 inhibitors. Bioorg Chem. 2026 Mar;170:109506.  [Content Brief]