Deltafluorine

Chemical Structure : Deltafluorine

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货号: PC-25958Not For Human Use, Lab Use Only.

Deltafluorine is a specific small molecule PDEδ inhibitor with ITC KD of 148 nM and binding IC50 of 25 nM, targeting the binding site glutamate p.E88 in PDEδ, impairs K-Ras signaling.

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生物&药学活性

Deltafluorine is a specific small molecule PDEδ inhibitor with ITC KD of 148 nM and binding IC50 of 25 nM, targeting the binding site glutamate p.E88 in PDEδ, impairs K-Ras signaling.
Deltafluorine impairs Ras pathway downstream of MAPK and Akt-mTOR pathways.
Deltafluorine (5 uM) shows rong inhibitory activity in KRAS-dependent pancreatic ductal adenocarcinoma cell lines PA-TU-8902 and MIA PaCa-2 cells with an average growth inhibition of 84 ± 2% and 87 ± 4%, respectively.
Deltafluorine (15 mg/kg i.p., q.d. for 21 days) reduces tumor growt in KrasLSL.G12D/wt;Trp53fl/fl (KP) mouse model.

物理化学性质&存储条件

分子量	677.29
分子式	C33H42ClFN4O4S2
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	N1-(4-chlorobenzyl)-N1-cyclopentyl-N4-((5-(fluoromethyl)-2,6-dimethylpyridin-3-yl)methyl)-N4-(piperidin-4-ylmethyl)benzene-1,4-disulfonamide

参考文献

1. Zhang R, et al. J Med Chem. 2026 Jan 7. doi: 10.1021/acs.jmedchem.5c02082.

Deltafluorine

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Deltafluorine

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