FTO degrader FP54

Chemical Structure : FTO degrader FP54

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货号: 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%.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	1173.26
分子式	C59H75Cl2N9O10S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(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

参考文献

1. Li W, et al. Sci Adv. 2025 Aug 15;11(33):eadv7648.