BETd-260 trifluoroacetate( ZBC 260 | ZBC260 | BETd 260 TFA )

Catalog No. M13421 CAS No. 2140289-21-8

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

BETd-260 trifluoroacetate
Note

Research use only, not for human use.
Brief 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.
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.
In Vitro

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In Vivo

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Synonyms

ZBC 260 | ZBC260 | BETd 260 TFA
Pathway

PROTACs
Target

PROTAC
Recptor

PROTAC
Research Area

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Indication

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CAS Number

2140289-21-8
Formula Weight

912.928
Molecular Formula

C45H47F3N10O8
Purity

>98% (HPLC)
Solubility

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SMILES

CCN1C(=CC(=N1)C2CC2)NC3=NC(=NC4=C3C5=CC(=C(C=C5N4)C6=C(ON=C6C)C)OC)C(=O)NCCCCCC7=C8CN(C(=O)C8=CC=C7)C9CCC(=O)NC9=O.C(=O)(C(F)(F)F)O
Chemical Name

4-((3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino)-7-(3,5-dimethylisoxazol-4-yl)-N-(5-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pentyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide 2,2,2-trifluoroacetate

1. Zhou B, et al. J Med Chem. 2017 Mar 24. doi: 10.1021/acs.jmedchem.6b01816.

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