Tubulin polymerization-IN-25

Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor of tubulin polymerization and farnesyl transferase (FTase) with IC50s of 1.11 μM and 0.39 μM, respectively. Tubulin polymerization-IN-25 displays cytotoxicity and excellent antitumor activity [1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

Signaling Pathways >> Metabolic Enzyme/Protease >> Farnesyl Transferase

IC50: 1.11 μM (Tubulin); 0.39 μM (FTase)[1]

Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor (MTI-FTI hybrids) acting on tubulin polymerization and on FTase[1]. Tubulin polymerization-IN-25 (10 μM, 48 h) inhibits cells growth and induces cell cytotoxicity on multiple cancer cell lines[1]. Cell Viability Assay[1] Cell Line: Leukemia cells: SR, CCRF-CEM, K-562; lung cancer cell CCRF-CEMNCI-H522; melanoma cell M14 Concentration: 10 μM Incubation Time: 48 hours Result: Inhibited cell growth. Cell Cytotoxicity Assay[1] Cell Line: NCI-H522 (lung cancer), COLO-205 and HT29 (colon cancer), SF-539 (human glioblastoma), MDA-MB-435 (melanoma), OVCAR-3 (ovarian cancer) and A498 (renal cancer) Concentration: 10 μM Incubation Time: 48 hours Result: Induced cell cytotoxicity.

[1]. Iuliana-Monica Moise, et al. Indolizine-phenothiazine hybrids as the first dual inhibitors of tubulin polymerization and farnesyltransferase with synergistic antitumor activity. Bioorg Chem. 2020 Oct; 103: 104184.