An eIF4E inhibitor
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Briciclib

Item No. 22989

Technical Information
Formal Name
2-methoxy-5-[[[(1E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl]methyl]-phenol 1-(dihydrogen phosphate)
CAS Number
865783-99-9
Synonyms
  • ON-014185
Molecular Formula
C19H23O10PS
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/ml
λmax
236, 308 nm
SMILES
COC1=CC=C(CS(/C=C/C2=C(OC)C=C(OC)C=C2OC)(=O)=O)C=C1OP(O)(O)=O
InChi Code
InChI=1S/C19H23O10PS/c1-25-14-10-17(27-3)15(18(11-14)28-4)7-8-31(23,24)12-13-5-6-16(26-2)19(9-13)29-30(20,21)22/h5-11H,12H2,1-4H3,(H2,20,21,22)/b8-7+
InChi Key
LXENKEWVEVKKGV-BQYQJAHWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    Briciclib is a water soluble derivative of ON 013100, a small molecule that binds to and inhibits eukaryotic translation initiation factor 4E (eIF4E).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jasani, N., Desai, B.J., Betzu, J.M., et alAbstract 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 Res. 75(15 Suppl), 1649 (2015).