货号	规格	价格	上海	北京	珠海	重庆	武汉
S87910-5mg买3赠1	99.70%	￥1020.00 S87910-5mg ￥1020.00 现货（买3赠1）	3 3	-	-	-	-
S87910-10mg买3赠1	99.70%	￥1530.00 S87910-10mg ￥1530.00 现货（买3赠1）	4 4	-	-	-	-
S87910-25mg买3赠1	99.70%	￥3060.00 S87910-25mg ￥3060.00 现货（买3赠1）	7 7	-	-	-	-
S87910-100mg	≥98%	￥9180.00 S87910-100mg ￥9180.00 2-3天	0 货期：2-3天	-	-	-	-

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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;Glucokinase; Autophagy

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：

-20℃

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。

参考文献

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