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 [1] [2].

FPFT-2216 (1 μM; 5 hours) is able to degrade PDE6D, in addition to its known targets IKZF1, IKZF3, and CK1α in MOLT4 cells [1]. FPFT-2216 (1 μM; 0 h, 2 h, 4 h, 6 h, 16 h, 24 h) shows complete degradation of PDE6D within 2 h, and the degradation of PDE6D persists for at least 24 h in MOLT4 cells [1]. FPFT-2216 (0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 1 μM; 4 h) exhibits 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 in MOLT4 cells [1]. FPFT-2216 does not impede the growth of KRAS G12C -dependent MIA PaCa-2 cells [1]. FPFT-2216 (10, 20, 40 μM; 14 or 24 h) highly up-regulates the production of IL-2 although it is less potent than that of Pomalidomide in Naive CD4 + T cells [2]. FPFT-2216 (10 μM; 14 or 24 h) degrades IKZF1 and CK-1α among ubiquitin–proteasomal degradative substrates of immunomodulatory drugs (IMiDs) in Naive CD4 + T cells [2]. Western Blot Analysis [1] 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 [1] 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.

FPFT-2216 (30 mg/kg; p.o. or i.p.) induces significant degradation of CK-1α, and IKZF1 in CRBN I391V mice [2]. Animal Model: CRBN I391V mice [2] Dosage: 30 mg/kg (solubilized in 0.5% carboxymethylcellulose/sodium and 0.25% Tween 80) Administration: p.o. or i.p. Result: Induced significant degradation of CK-1α, and IKZF1.

2367619-87-0

C12H12N4O3S

292.31

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years