BETd-260 (ZBC 260) (Synonyms: ZBC 260) |
Catalog No.GC32791 |
BETd-260 (ZBC 260) (ZBC 260) es un PROTAC conectado por ligandos para Cereblon y BET, con tan solo 30 pM contra la proteÍna BRD4 en la lÍnea celular de leucemia RS4;11. BETd-260 (ZBC 260) suprime de forma potente la viabilidad celular e induce de forma sÓlida la apoptosis en células de carcinoma hepatocelular (HCC).
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Cas No.: 2093388-62-4
Sample solution is provided at 25 µL, 10mM.
BETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 30 pM against BRD4 protein in RS4;11 leukemia cell line.
BETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 30 pM for BRD4 protein in RS4;11 leukemia cell line. BETd-260 (ZBC260; Compound 23) shows inhibitory activity against the growth of RS4;11 leukemia cells and MOLM-13 cells with IC50s of 51 pM and 2.2 nM, respectively, and induces apoptosis in both RS4;11 and MOLM-13 cell lines at 3-10 nM[1].
BETd-260 (5 mg/kg, i.v., every other day, thrice a week for 3 weeks) causes rapid tumor regression with a maximum of >90% regression in mice bearing RS4;11 xenograft tumors, and with no body weight loss or other signs of toxicity in mice. BETd-260 (5 mg/kg, i.v.) degrades the BRD2, BRD3, and BRD4 proteins for more than 24 h, with robust cleavage of PARP and caspase-3, and strong down-regulation of c-Myc protein in RS4;11 xenograft mice model[1].
[1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
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