| 产品描述： | KAN0438757 是一种有效的、选择性的代谢激酶 PFKFB3 (6-Phosphofructo-2-Kinase/Fructose-2,6-Biphosphatase 3) 的抑制剂，对于PFKFB3和PFKFB4的IC50值分别为0.19 μM和3.6 μM |
| 靶点： |
PFKFB3(Cell-free assay):0.19 μM; PFKFB4(Cell-free assay):3.6 μM |
| 体外研究： |
A PFKFB3 inhibitor, KAN0438757, which selectively inhibits proliferation of transformed cells while sparing non-transformed cells. Inhibition of PFKFB3 enzymatic activity by KAN0438757 impairs IR-induced recruitment of ribonucleotide reductase (RNR) M2 and deoxynucleotide incorporation upon DNA repair |
| 体内研究： |
In vivo administration of KAN0438757 in mice is well tolerated and does not trigger major systemic or toxic alterations |
| 细胞实验： |
Cell lines: U2OS cells Concentrations: 10 μM Incubation Time: 6 h Method: Confocal analysis of IR-induced foci of RAD51 or RPA32 in U2OS cells following treatment with DMSO or 10 μM KAN757 (6 h), subjected to IR (6 Gy, 2 h recovery), or left untreated. HR activity after treatment of U2OS DR-GFP cells with indicated inhibitors as assessed by FACS analysis. |
| 动物实验： |
Animal Models: C57BL6/N mice Dosages: 10, 25, 50 mg/kg Administration: i.p. |
| 参考文献： |
1. Nina M S Gustafsson, et al. Targeting PFKFB3 radiosensitizes cancer cells and suppresses homologous recombination. Nat Commun. 2018 Sep 24;9(1):3872. 2. De Oliveira T, et al. Effects of the Novel PFKFB3 Inhibitor KAN0438757 on Colorectal Cancer Cells and Its Systemic Toxicity Evaluation In Vivo. Cancers (Basel). 2021 Feb 28;13(5):1011. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.235 ml |
11.175 ml |
22.35 ml |
| 5 mM |
0.447 ml |
2.235 ml |
4.47 ml |
| 10 mM |
0.223 ml |
1.117 ml |
2.235 ml |
| 50 mM |
0.045 ml |
0.223 ml |
0.447 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京