BETd-260 trifluoroacetate

Names

[ 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

Related Compounds

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