Phenol, 2-Methoxy-5-[[[(1E)-2-(2,4,6-triMethoxyphenyl)ethenyl]sulfonyl]Methyl]-, 1-(dihydrogen phosphate)

Description

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.

Uses

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

IC 50

eIF4

References

[1] NEEL JASANI. Abstract 1649: Potent anticancer activity of an orally bioavailable small molecule, ON 013100, and its water soluble derivative, briciclib, a clinical-stage eIF4E-targeted agent[J]. Cancer research, 2015, 75 1: 1649-1649. DOI: 10.1158/1538-7445.am2015-1649