计算溶液所需的质量、体积或浓度。
概述
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
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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 AnalysisCell 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.
In Vivo
FPFT-2216 (30 mg/kg; p.o. or i.p.) induces significant degradation of CK-1α, and IKZF1 in CRBN I391V mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CRBN I391V miceDosage: 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.
Form:Solid
IC50& Target:PDE6D CK1α IKZF1 IKZF3
规格
规格或纯度
≥99%
英文名称
FPFT-2216
生化机理
FPFT-2216是一种 "分子胶 "化合物，能降解磷酸二酯酶6D（PDE6D）、锌指转录因子Ikaros（IKZF1）、Aiolos（IKZF3）和酪蛋白激酶1α（CK1α）。FPFT-2216 可用于癌症和炎症性疾病的研究
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
292.31
高级数据
化学和物理性质
溶解性
DMSO : 100 mg/mL (342.10 mM; Need ultrasonic)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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