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.
For research use only. We do not sell to patients.
- Formula: C21H16BrN3O3S
- Molecular Weight:470.34
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All VEGFR Isoforms
More
Biological Activity
|
VEGFR2 1.94 μM (IC50) |
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.
-
Cell Line:HCT-116 human colon cancer cells
-
Concentration:2 μM, 7 μM, 15 μM
-
Incubation Time:24 h
-
Result: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.
Chemical Information
-
Molecular Weight 470.34
-
Formula C21H16BrN3O3S
-
SMILES
O=C1N(C2=NC(C3=CC=C(Br)C=C3)=CS2)C(N)=C(C(OCC)=O)C4=CC=CC=C41
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VEGFR-2-IN-81 Related Classifications
HY-181493 Related Classifications
Powered by Bioz
- VEGFR-2-IN-81
- VEGFR
- Reactive Oxygen Species (ROS)
- Apoptosis
- HEK-293 cells
- HEPG-2 human hepatocellular carcinoma cells
- HCT-116 human colon cancer cells
- A549 human lung cancer cells
- VEGFR-2 inhibitor
- MCF-7 human breast cancer cells
- selective cytotoxicity
- induce apoptosis
- elevate intracellular ROS
- reduce mitochondrial transmembrane potential
- Inhibitor
- inhibitor
- inhibit