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FD223

    
10mM in DMSO

源叶(MedMol)
V57475 一键复制产品信息
2050524-24-6
C17H12ClN5O2S
385.83
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
V57475-1ml
10mM in DMSO

¥2210.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML.
靶点: PI3Kδ:1 nM (IC50); PI3Kα:51 nM (IC50); PI3Kβ:29 nM (IC50); PI3Kγ:37 nM (IC50)
体内研究: FD223 exhibits notable anti-proliferative activities in the p110δ-positive AML cell lines HL-60, MOLM-16, EOL-1 and KG-1, with the IC50 of 2.25 μM, 0.87 μM, 2.82 μM, and 5.82 μM, respectively. FD223 shows weak anti-proliferative activity against p110δ unexpressed MM.1R cell line, with the IC50 value of 23.13 μM.
FD223 (MOLM-16 cells; 0.1-5 μM; 16 hours) dose-dependently reduces phosphorylation of Akt (Ser473), which is consistent with the positive control Idelalisib, illustrating that the activity of PI3K/Akt pathway in MOLM-16 cell is blocked.
FD223 (MOLM-16 cells; 24 hours; 1-5 μM) arrests the cell cycle at the G1 phase similar to that of positive control Idelalisib.
FD223 (1-5 μM; 48 hours) dose-dependently induces cellular apoptosis.
参考文献: 1. Yang C, et al. Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation [published online ahead of print, 2021 Jun 21]. Eur J Med Chem. 2021;223:113661.
 
保存条件: -80°C 6个月;-20°C 1个月
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.592 ml 12.959 ml 25.918 ml
5 mM 0.518 ml 2.592 ml 5.184 ml
10 mM 0.259 ml 1.296 ml 2.592 ml
50 mM 0.052 ml 0.259 ml 0.518 ml
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参考文献

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摩尔浓度计算器

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