| 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 |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |