BETd-260 trifluoroacetate
Names
[ CAS No. ]:
2140289-21-8
[ Name ]:
BETd-260 trifluoroacetate
Biological Activity
[Description]:
BETd-260 trifluoroacetate (ZBC260, BETd 260 TFA) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL; effectively degrades BRD4 protein at 30 pM in the RS4;11 leukemia cell line, achieves an IC50 of 51 pM in inhibition of RS4;11 cell growth and induces rapid tumor regression in vivo against RS4;11 xenograft tumors.
[References]
References 1. Zhou B, et al. J Med Chem. 2017 Mar 24. doi: 10.1021/acs.jmedchem.6b01816. View Related Products by Target PROTAC
Chemical & Physical Properties
[ Molecular Formula ]:
C45H47F3N10O8
[ Molecular Weight ]:
912.928