Multi-kinase-IN-1

Multi-kinase-IN-1 (Compound 11k) is a potent kinase inhibitor with antitumor activity. Multi-kinase-IN-1 induces cell apoptosis, and can be studied for colorectal cancer[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> TAM Receptor

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR

c-Met:0.382 μM (IC50)

PDGFRα:0.384 μM (IC50)

Ron:0.122 μM (IC50)

c-Src:0.421 μM (IC50)

AXL:0.632 μM (IC50)

Multi-kinase-IN-1 (Compound 11k) (0-5 µg/mL, 0-72 h) induces antiproliferation and cytotoxicity in a dose- and time-dependent manner in HT-29 cells, and is much less toxic to normal colorectal mucosa epithelial cells[1]. Multi-kinase-IN-1 (0-3 µg/mL, 0-72 h) induces cell apoptosis in a time- and dose-dependent manner[1]. Multi-kinase-IN-1 (0-3 µg/mL, 48 h) slightly induces cell cycle arrest in G2/M phase[1]. Cell Proliferation Assay[1] Cell Line: HT-29 (human colon cancer cell) and FHC (normal colorectal mucosa epithelial cells) Concentration: 0.56, 1.67, and 5 µg/mL for HT-29, 10 µg/mL for FHC Incubation Time: 0-72 h Result: Led to significant cytotoxicity in a dose- and time-dependent manner in HT-29 cells. Showed low toxicity in FHC cells. Apoptosis Analysis[1] Cell Line: HT-29 Concentration: 0.3, 1, and 3 µg/mL Incubation Time: 0-72 h Result: Induced cell apoptosis in a time- and dose-dependent manner. Cell Cycle Analysis[1] Cell Line: HT-29 Concentration: 0.3, 1, and 3 µg/mL Incubation Time: 48 h Result: Slightly induced cell cycle arrest with a G2/M percentage of 4.4% at 3.0 mg/mL compared to 0.1% DMSO (2.4%).

[1]. Yuting Zhou, et al. Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. Eur J Med Chem. 2020 Oct 15;204:112643.