Chemical Structure : PLK4 PROTAC SP27
CAS No.:
3034805-75-6
PLK4 PROTAC SP27
Catalog No.: PC-25887Not For Human Use, Lab Use Only.
PLK4 PROTAC SP27 is a potent, selective PLK4 proteolysis targeting chimera (PROTAC) degrader with binding IC50 of 8.4 nM for PLK4, DC50 of 19.5 nM in MCF-7 cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
PLK4 PROTAC SP27 is a potent, selective PLK4 proteolysis targeting chimera (PROTAC) degrader with binding IC50 of 8.4 nM for PLK4, DC50 of 19.5 nM in MCF-7 cells.
SP27 showed strong antiproliferative activity on MCF-7 cells with IC50 of 73 nM.
SP27 killed TRIM37-amplified MCF-7 cells more efficiently than PLK4 inhibitor CZS-035.
SP27 induced the PLK4 degradation through CRBN-dependent ubiquitin-proteasome pathway.
SP27 (1 nM-1 uM) reduced the inactivation of FBXW5 and increased SAS-6 degradation in a concentration-dependent manner in MCF-7 cells.
SP27 could induce cell apoptosis in MCF-7 cells.
SP27 (20 mg/kg once every other day through i.p. injection) demonstrated n vivo antitumor activity in female nu/nu mice bearing MCF-7 xenografts.
Physicochemical Properties
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M.Wt
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806.84
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Formula
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C40H40F2N12O5
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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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5-(4-(4-(6-((2,4-Difluorobenzyl)amino)-4-((5-methyl-1H-pyrazol-3-yl)amino)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carbonyl)piperidin-1-yl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
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References
1. Sun Y, et, al. J Med Chem. 2023 Jun 22;66(12):8200-8221.
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