FPFT-2216

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

FPFT-2216 是一种“分子胶水”化合物，可降解磷酸二酯酶 6D (PDE6D)、锌指转录因子 Ikaros (IKZF1)、Aiolos (IKZF3) 和酪蛋白激酶 1α (CK1α)。FPFT-2216 可用于癌症和炎症疾病的研究。

FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease.

Western Blot Analysis Cell Line:MOLT4 cells Concentration:1 μM Incubation Time:0 h, 2 h, 4 h, 6 h, 16 h, 24 h Result:Showed complete degradation of PDE6D within 2 h, and the degradation of PDE6D persisted for at least 24 h.Western Blot Analysis Cell Line:MOLT4 cells Concentration:0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 1 μM Incubation Time: 4 h Result:Exhibited over 50% degradation of PDE6D at a dose of 8 nM, while maximum degradation of PDE6D along with IKZF1, IKZF3, and CK1α at a dose of 200 nM.

Animal Model:CRBNI391V mice Dosage:30 mg/kg (solubilized in 0.5% carboxymethyl cellulose/sodium and 0.25% Tween 80) Administration:p.o. or i.p.Result:Induced significant degradation of CK-1α, and IKZF1.

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Metabolic Enzyme/Protease

Casein Kinase

Casein Kinase | Molecular Glues | PDE

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2367619-87-0

292.31

C12H12N4O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (342.10 mM; 超声助溶 )

COc1cscc1-c1cn(nn1)C1CCC(=O)NC1=O

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(-20℃)

With Ice Pack

≥ 2 years