Chemical Structure : XZ739
CAS No.:
2365172-19-4
XZ739
Catalog No.: PC-24379Not For Human Use, Lab Use Only.
XZ739 is a potent, CRBN-dependent PROTAC BCL-XL degrader with DC50 of 2.5 nM (MOLT-4 cells), reduces MOLT-4 cell viability with IC50 of 10.1 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
XZ739 is a potent, CRBN-dependent PROTAC BCL-XL degrader with DC50 of 2.5 nM (MOLT-4 cells), reduces MOLT-4 cell viability with IC50 of 10.1 nM.
XZ739 dose-dependently induced BCL-XL degradation in MOLT-4 cells, which can be abrogated by proteasome inhibitor MG-132.
XZ739 shows improved selectivity because of its low activity in inducing BCL-XL degradation in human platelets, and the remaining cytotoxicity to human platelets mainly depends on BCL-XL inhibition.
XZ739 does not affect IKZF1 and IKZF3 protein levels, has >100-fold selectivity for MOLT-4 cells over human platelets.
Physicochemical Properties
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M.Wt
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1349.99
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Formula
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C65H76ClF3N8O12S3
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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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4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-(((15R)-1-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-12-methyl-16-(phenylthio)-3,6,9-trioxa-12-azahexadecan-15-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide
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References
1. Zhang X, et al. Eur J Med Chem. 2020 Apr 15;192:112186.
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