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Briciclib

Names

[ CAS No. ]:
865783-99-9

[ Name ]:
Briciclib

[Synonym ]:
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)

Biological Activity

[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.


[Related Small Molecules]

Silvestrol | eIF4E/eIF4G Interaction Inhibitor, 4EGI-1 | 4E1RCat | 4E2RCat | GCN2iB | CCT020312

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
762.6±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C19H23O10PS

[ Molecular Weight ]:
474.419

[ Flash Point ]:
415.0±35.7 °C

[ Exact Mass ]:
474.074951

[ PSA ]:
156.01000

[ LogP ]:
0.89

[ Appearance of Characters ]:
white solid

[ Vapour Pressure ]:
0.0±2.7 mmHg at 25°C

[ Index of Refraction ]:
1.578

[ Storage condition ]:
-20℃

Related Compounds