CAS 865783-99-9|Briciclib

Introduction:Basic information about CAS 865783-99-9|Briciclib, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameBriciclib
CAS Number865783-99-9Molecular Weight474.419
Density1.4±0.1 g/cm3Boiling Point762.6±70.0 °C at 760 mmHg
Molecular FormulaC19H23O10PSMelting Point/
MSDS/Flash Point415.0±35.7 °C

Names

Name2-Methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)vinyl]sulfonyl}methy l)phenyl dihydrogen phosphate
SynonymMore Synonyms

Briciclib BiologicalActivity

DescriptionBriciclib is a water soluble derivative of ON 013100, and has the potential in targeting eIF4E for solid cancers.
Related CatalogSignaling Pathways >>Cell Cycle/DNA Damage >>Eukaryotic Initiation Factor (eIF)Research Areas >>Cancer
Target

eIF4E[1]

In VitroBriciclib 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.

Chemical & Physical Properties

Density1.4±0.1 g/cm3
Boiling Point762.6±70.0 °C at 760 mmHg
Molecular FormulaC19H23O10PS
Molecular Weight474.419
Flash Point415.0±35.7 °C
Exact Mass474.074951
PSA156.01000
LogP0.89
Appearance of Characterswhite solid
Vapour Pressure0.0±2.7 mmHg at 25°C
Index of Refraction1.578
InChIKeyLXENKEWVEVKKGV-BQYQJAHWSA-N
SMILESCOc1cc(OC)c(C=CS(=O)(=O)Cc2ccc(OC)c(OP(=O)(O)O)c2)c(OC)c1
Storage condition-20℃

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)
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