Chemical Structure : DBt-10
CAS No.:
DBt-10
(DCAF1-BTK-PROTAC)
Catalog No.: PC-21641Not For Human Use, Lab Use Only.
DBt-10 is a potent BTK-specific DCAF1 PROTAC with TR-FRET IC50 of 136 nM, potently degrades BTK with DC50 of 137 nM in TMD8 BTK-GFP/mCherry cell-based assays.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
DBt-10 (DCAF1-BTK-PROTAC) is a potent BTK-specific DCAF1 PROTAC with TR-FRET IC50 of 136 nM, potently degrades BTK with DC50 of 137 nM in TMD8 BTK-GFP/mCherry cell-based assays.
DBt-10 (DCAF1-BTK-PROTAC) displays minimal off-target toxicities and high selectivity for BTK.
DCAF1 is an alternative essential ligase for the application of PROTACs in biological contexts where VHL is not expressed, e.g., in renal cell carcinoma.
DBt-10 (DCAF1-BTK-PROTAC) shows potent degradation of BTK, consistent with retention of DCAF1 protein levels independent of CRBN status.
Physicochemical Properties
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M.Wt
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1277.99
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Formula
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C68H86ClFN16O6
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(3-(6-(1-(2-(4-(2-(5-(4-(4-((2-aminoethyl)amino)-2-(1-(4-chlorophenyl)cyclohexyl)quinazolin-7-yl)piperazin-1-yl)-5-oxopentanamido)ethyl)-1-oxa-4,9-diazaspiro[5.5]undecan-9-yl)-2-oxoethyl)-1Hpyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-3-hydroxy-3-neopentylazetidine-1-carboxamide
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References
1. Schröder M, et al. Nat Commun. 2024 Jan 4;15(1):275.
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