Amsilarotene (TAC-101) is a retinobenzoic acid with potential antineoplastic activity, shows selective affinity for RARα with binding Ki of 2.4 nM.
Amsilarotene inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependent kinase (CDK) inhibitors, resulting in cell cycle arrest.
Amsilarotene also causes a cytotoxic decline in cyclin A and thymidylate synthase expression.
Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells.
