Chemical Structure : FTO PROTAC QP73
CAS No.:
FTO PROTAC QP73
Catalog No.: PC-23898Not For Human Use, Lab Use Only.
FTO PROTAC QP73 is a first-in-class PROTAC degrader for the RNA demethylase FTO, efficiently induces FTO protein degradation in a dose-, time-, cereblon (CRBN)-, and proteasome-dependent manner in AML cells (DC50=34.9 nM, NB4 cells).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
FTO PROTAC QP73 is a first-in-class PROTAC degrader for the RNA demethylase FTO, efficiently induces FTO protein degradation in a dose-, time-, cereblon (CRBN)-, and proteasome-dependent manner in AML cells (DC50=34.9 nM, NB4 cells).
QP73 (100 nM) decreased FTO abundance by 91% in NB4 cells, FTO degradation by QP73 in MV4-11 AML cells has DC50 of 65.9 nM.
QP73 exerts high antileukemic activity by targeting FTO in AML cells with low nanomolar IC50 values (12.9-108.1 nM), inhibits the clone formation of NB4 cells
QP73 markedly increases the m6A abundance on mRNA in a dose-dependent manner in NB4 and MV4-11 cells.
QP73 degrades FTO through a CRBN-dependent proteasomal degradation mechanism.
QP73 (2.5 or 5 mg/kg) exhibits potent suppression cancer growth in NB4 AML xenograft mouse model.
Physicochemical Properties
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M.Wt
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739.20
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Formula
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C39H36ClFN6O6
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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-((7-(2-((2-chloro-4-(3,5-dimethylisoxazol-4-yl)-6-fluorophenyl)amino)benzoyl)-7-azaspiro[3.5]nonan-2-yl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
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References
1. Liu L, et al. Acta Pharm Sin B. 2024 Dec;14(12):5382-5392.
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