FTO PROTAC QP73

Chemical Structure : FTO PROTAC QP73

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货号: PC-23898Not For Human Use, Lab Use Only.

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 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.

物理化学性质&存储条件

分子量	739.20
分子式	C39H36ClFN6O6
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	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

参考文献

1. Liu L, et al. Acta Pharm Sin B. 2024 Dec;14(12):5382-5392.

FTO PROTAC QP73

生物&药学活性

物理化学性质&存储条件

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FTO PROTAC QP73

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