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Briciclib

Catalog No.: 611917
Cas No.: 865783-99-9
Purity : 98% 
611917 - Briciclib | CAS 865783-99-9

Catalog number : 611917

CAS number : 865783-99-9

分子式 : C19H23O10PS 

分子量 : 474.42 

Iupac 化学名称 : Briciclib 

Smile : COc1ccc(cc1OP(=O)(O)O)CS(=O)(=O)/C=C/c2c(cc(cc2OC)OC)OC

InChiKey : LXENKEWVEVKKGV-BQYQJAHWSA-N

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同义词ON-014185; ON014185; ON 014185 
英文同义词ON-014185; ON014185; ON 014185 
分子式C19H23O10PS 
分子量474.42 
外观crystalline solid 
纯度98% 
可溶性Soluble in DMSO 
存储3 years -20ºCpowder 
运输条件Shipped under ambient temperature as non-hazardous chemical. 
SmileCOc1ccc(cc1OP(=O)(O)O)CS(=O)(=O)/C=C/c2c(cc(cc2OC)OC)OC
InChiKeyLXENKEWVEVKKGV-BQYQJAHWSA-N
InChiInChI=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+
MDLMFCD22665751
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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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