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865783-99-9

865783-99-9 structure
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
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.

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 white solid
Vapour Pressure 0.0±2.7 mmHg at 25°C
Index of Refraction 1.578
Storage condition -20℃