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BETd-260 trifluoroacetate

Chemical Structure : BETd-260 trifluoroacetate

CAS No.: 2140289-21-8

BETd-260 trifluoroacetate (ZBC260, BETd260 TFA)

Catalog No.: PC-60103Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.
BETd-260 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.
BETd-260 induces rapid tumor regression in vivo against RS4;11 xenograft tumors.

Physicochemical Properties

M.Wt 912.928
Formula C45H47F3N10O8
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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

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