865783-99-9

865783-99-9 structure

Name: Briciclib
Chemical Name: 2-Methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)vinyl]sulfonyl}methy l)phenyl dihydrogen phosphate
CAS Number: 865783-99-9
Molecular Formula: C₁₉H₂₃O₁₀PS
Molecular Weight: 474.419
Catalog: Signaling Pathways Cell Cycle/DNA Damage Eukaryotic Initiation Factor (eIF)
Create Date: 2018-05-23 08:00:00
Modify Date: 2024-01-04 12:17:43
Briciclib is a water soluble derivative of ON 013100, and has the potential in targeting eIF4E for solid cancers.

Name	2-Methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)vinyl]sulfonyl}methy l)phenyl dihydrogen phosphate
Synonyms	2-Methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)vinyl]sulfonyl}methyl)phenyl dihydrogen phosphate ON 014185 Phenol, 2-methoxy-5-[[[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]-, dihydrogen phosphate Briciclib 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, and has the potential in targeting eIF4E for solid cancers.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> Eukaryotic Initiation Factor (eIF) Research Areas >> Cancer
Target	eIF4E[1]
In Vitro	Briciclib has the potential in targeting eIF4E. Briciclib shows inhibitory activity against the proliferation of mantle cell leukemia (EKO-1 and MINO), breast (MCF7 and MDA-MB-231), gastric (AGS), and esophageal (OE19, OE33, and FLO-1) cancer cell lines with GI50s of 9.8-12.2 nM, and with no toxicity on normal endothelial cells. Briciclib dose-dependently reduces the expression of cyclin D1 and c-Myc in breast and MCL cancer cell lines within 8 hours[1].
References	[1]. Neel Jasani, et al. 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. Cancer Research. August 2015, Volume 75, Issue 15.