Chemical Structure : FTO degrader FP54
CAS No.:
FTO degrader FP54
Catalog No.: PC-25493Not For Human Use, Lab Use Only.
FTO degrader FP54 is a selective PROTAC degrader of fat mass and obesity-associated protein (FTO) with DCof 0.68 μM in NB4 cells and 0.71 μM in MOLM-13 cells, Dmax>95%.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
FTO degrader FP54 is a selective PROTAC degrader of fat mass and obesity-associated protein (FTO) with DCof 0.68 μM in NB4 cells and 0.71 μM in MOLM-13 cells, Dmax>95%.
FP54 does not induce degradation of other RNA m6A effector proteins, including YTHDF2, METTL3, and ALKBH5 in NB4 cells.
FP54 induces FTO degradation primarily through a mechanism that relies on the recruitment of the VHL E3 ligase complex and subsequent ubiquitin-proteasome–mediated degradation.
FP54 selectively inhibits proliferation and promotes apoptosis of AML cells with IC50 values ranging from 0.48 to 2.44 uM.
FP54 down-regulates ribosome biogenesis–related pathways in AML.
FP54 (25 mg/kg) markedly reduced the leukemia burden and delayed the onset of AML cells in AML mouse models.
Physicochemical Properties
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M.Wt
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1173.26
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Formula
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C59H75Cl2N9O10S
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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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(isobutyryloxy)methyl 2-((2,6-dichloro-4-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-6-(4-(2-((7-(((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-7-oxoheptyl)amino)-2-oxoethyl)piperazin-1-yl)benzoate
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References
1. Li W, et al. Sci Adv. 2025 Aug 15;11(33):eadv7648.
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