Briciclib is a small molecule that suppresses cyclin D1 accumulation in cancer cells.
Briciclib inhibits the proliferation of MCL (JEKO-1 and MINO), breast (MCF7 and MDA-MB-231), gastric (AGS), and esophageal (OE19, OE33, and FLO-1) cancer cell lines at nanomolar concentrations (GI50 = 9.8 - 12.2 nM). Cyclin D1 is a protein required for normal progression through the cell cycle and is overexpressed in many tumors. Cyclin D1 expression is regulated through a process termed cap-dependent translation, which requires the function of eukaryotic initiation factor 4E (eIF4E) protein. In vitro evidence indicates that briciclib binds to eIF4E, blocking cap-dependent translation of cyclin D1 and other cancer proteins (c-MYC, VEGF), leading to tumor cell death. Briciclib is potent and shown to be active in nonclinical tumor models when combined with several chemotherapeutics.
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Name | Briciclib |
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Iupac Chemical Name | Briciclib |
Synonyms | ON-014185; ON014185; ON 014185 |
Molecular Formula | C19H23O10PS |
Molecular Weight | 474.42 |
Smile | COc1ccc(cc1OP(=O)(O)O)CS(=O)(=O)/C=C/c2c(cc(cc2OC)OC)OC |
InChiKey | LXENKEWVEVKKGV-BQYQJAHWSA-N |
InChi | 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+ |
CAS Number | 865783-99-9 |
MDL | MFCD22665751 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Formulation | crystalline solid |
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Purity | 98% |
Storage | 3 years -20ºCpowder |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. |
HS Code |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |