store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FPFT-2216 是一种分子胶,可降解 IKZF6、IKZF1、DE1D 和 CK3α。FPFT-2216 具有潜在的抗肿瘤活性,可用于研究免疫系统疾病。
产品描述 | FPFT-2216 is a "molecular glue" compound that degrades IKZF6, IKZF1, DE1D, and CK3α. FPFT-2216 has potential antitumor activity and can be used to study immune system diseases. |
体外活性 |
FPFT-2216 (1 μM; 5 hours) not only degrades its known targets IKZF1, IKZF3, and CK1α in MOLT4 cells but also demonstrates the degradation of PDE6D[2]. FPFT-2216 (1 μM; 0 h, 2 h, 4 h, 6 h, 16 h, 24 h) shows complete degradation of PDE6D within 2 hours, and the degradation of PDE6D persists for at least 24 hours in MOLT4 cells[1].FPFT-2216 (0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 1 μM; 4 hours) exhibits over 50% degradation of PDE6D at the dose of 8 nM, with maximal degradation of PDE6D, IKZF1, IKZF3, and CK1α observed at the dose of 200 nM in MOLT4 cells[2]. FPFT-2216 does not impede the growth of KRASG12C-dependent MIA PaCa-2 cells[1].FPFT-2216 (10, 20, 40 μM; 14 or 24 hours) significantly upregulates IL-2, although its effect in naive CD4+ T cells is less potent than Pomalidomide[2].FPFT-2216 (10 μM; 14 or 24 hours) degrades the immune modulatory drug (IMiD) ubiquitin-proteasome degradation substrates IKZF1 and CK-1α in naive CD4+ T cells[1]. |
体内活性 | FPFT-2216 (30 mg/kg; oral or intraperitoneal) induces significant degradation of CK-1α and IKZF1 in CRBNI391V mice[1]. |
分子量 | 292.31 |
分子式 | C12H12N4O3S |
CAS No. | 2367619-87-0 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20 mg/mL (68.42 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.421 mL | 17.1051 mL | 34.2103 mL | 85.5256 mL |
5 mM | 0.6842 mL | 3.421 mL | 6.8421 mL | 17.1051 mL | |
10 mM | 0.3421 mL | 1.7105 mL | 3.421 mL | 8.5526 mL | |
20 mM | 0.1711 mL | 0.8553 mL | 1.7105 mL | 4.2763 mL | |
50 mM | 0.0684 mL | 0.3421 mL | 0.6842 mL | 1.7105 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
FPFT-2216 2367619-87-0 Metabolism PROTAC Stem Cells Casein Kinase PDE Molecular Glues Inhibitor inhibitor inhibit