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Chemical Structure : BETd-260 trifluoroacetate
CAS No.: 2140289-21-8
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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|---|---|---|---|
| 1 mg | $198 | In stock | |
| 5 mg | $358 | In stock | |
| 10 mg | $588 | In stock | |
| 25 mg | Get quote |
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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.
| M.Wt | 912.928 | |
| Formula | C45H47F3N10O8 | |
| 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 2,2,2-trifluoroacetate |
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1. Zhou B, et al. J Med Chem. 2017 Mar 24. doi: 10.1021/acs.jmedchem.6b01816.
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