Tubulin/CDC5L-IN-1 is a dual inhibitor targeting Tubulin and CDC5L. It specifically targets CDCL5 with a KD value of 103.7 μM. This compound inhibits the proliferation of various cancer cells and induces G2/M phase arrest. Tubulin/CDC5L-IN-1 also promotes apoptosis (apoptosis) and the production of reactive oxygen species (ROS), and possesses anti-angiogenic properties. It is useful in cancer research, including studies on colon cancer.

Tubulin/CDC5L-IN-1 (Compound 11i) effectively inhibits the proliferation of HeLa, HCT 116, A2780, and A549 cells with IC50 values of 0.046, 0.035, 0.096, and 0.112 μM, respectively. It demonstrates antiproliferative effects in drug-resistant cancer cells with IC50 values ranging from 0.089 to 0.172 μM. The compound inhibits microtubule assembly at concentrations of 1-100 μM over 0-30 minutes, showing an IC50 of 28.8 μM. Tubulin/CDC5L-IN-1 suppresses colony formation in HeLa and HCT 116 cells at concentrations between 0.125-0.05 μM over 24 hours. It induces G2/M phase arrest in HCT 116 cells at 0.125-0.1 μM for 12 hoursand promotes apoptosis and reactive oxygen species (ROS) production in HCT 116 cells at 0.05-0.2 μM for 24 hours. Additionally, it inhibits the formation of capillary-like structures in human umbilical vein endothelial cells (HUVECs) within 4 hours at concentrations of 0.05-0.2 μM. Tubulin/CDC5L-IN-1 also inhibits DNA-dependent protein kinase and cell division cycle 7 at a concentration of 5 μM.

Tubulin/CDC5L-IN-1 (Compound 11i), administered via intraperitoneal injection every two days at doses of 7.5-20 mg/kg, effectively inhibits tumor growth in HCT116 xenograft mouse models.