865783-99-9

Briciclib is a water soluble derivative of ON 013100, a small molecule that binds to and inhibits eukaryotic translation initiation factor 4E (eIF4E). Briciclib inhibits proliferation of JEKO-1 and Mino mantle cell leukemia (MCL), MCF-7 and MDA-MB-231 breast, AGS gastric, and OE19, OE33, and LFO-1 esophageal cancer cell lines with GI₅₀ values ranging from 9.8 to 12.2 nM. It reduces expression of cyclin D1 and c-Myc, markers of eIF4E activity, in breast and MCL cancer cell lines in a dose-dependent manner. Briciclib also induces expression of the pro-apoptotic proteins p53 and cleaved caspase-3.

Briciclib is a useful organic intermediate employed in the synthesis of [[(phenylmethyl)sulfonyl]ethenyl]benzene derivatives with anticancer activity.

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