FPFT-2216,2367619-87-0

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FPFT-2216

CAS No. : 2367619-87-0

MCE 国际站：FPFT-2216

产品活性：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。

研究领域：Metabolic Enzyme/Protease  |  Stem Cell/Wnt  |  Cell Cycle/DNA Damage  |  PROTAC

作用靶点：Phosphodiesterase (PDE)  |  Casein Kinase  |  Molecular Glues

In Vitro: FPFT-2216 (1 μM; 5 hours) is able to degrade PDE6D, in addition to its known targets IKZF1, IKZF3, and CK1α in MOLT4 cells.
?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.
?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.
?FPFT-2216 does not impede the growth of KRAS^G12C-dependent MIA PaCa-2 cells.
?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.
?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.

In Vivo: FPFT-2216 (30 mg/kg; p.o. or i.p.) induces significant degradation of CK-1α, and IKZF1 in CRBN^I391V mice.

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