BETd-260 (ZBC 260) (Synonyms: ZBC 260) |
Catalog No.GC32791 |
BETd-260(ZBC 260)(ZBC 260)은 RS4;11 백혈병 세포주에서 BRD4 단백질에 대해 30pM만큼 낮은 Cereblon 및 BET용 리간드로 연결된 PROTAC입니다. BETd-260(ZBC 260)은 세포 생존력을 강력하게 억제하고 간세포 암종(HCC) 세포에서 세포자멸사를 강력하게 유도합니다.
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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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