Chemical Structure : BETd-260
CAS No.: 2093388-62-4
Catalog No.: PC-60102Not For Human Use, Lab Use Only.
BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.
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BETd-260 (ZBC260, BETd260) 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.
M.Wt | 798.905 | |
Formula | C43H46N10O6 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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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 |
1. Zhou B, et al. J Med Chem. 2017 Mar 24. doi: 10.1021/acs.jmedchem.6b01816.
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