Briciclib

Briciclib is a water soluble derivative of ON 013100, a small molecule that binds to and inhibits eukaryotic translation initiation factor 4E (eIF4E). 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.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: 474.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml. lambdamax: 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.