切换导航

FK866 (APO866)

现货
Catalog No.
A4381
NAMPT抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 650.00
现货
5mg
¥ 600.00
现货
10mg
¥ 1,100.00
现货
25mg
¥ 2,500.00
现货
50mg
¥ 3,900.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

FK866 is an inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 values ranging between 0.09nM and 27.2nM [1].

NAD plays a vital role in numerous biochemical and biologic processes. Targeting NAD synthesis is thought to be a selective manner to kill cancer cells since cancer cells have a higher rate of NAD turnover compared with normal cells. In the in vitro MTT assay using a panel of 41 human hematologic cancer

cell lines, most cancer cells are sensitive to low concentrations of FK866. Among these cancer cells, AML cells are most sensitive. FK866 is shown selective to human hematologic malignant cells and the normal human HPCs are resistant to FK866 treatment. It is found that FK866 induces cell death in a caspase-independent pathway but in a dose-dependent manner to induce mitochondrial membrane depolarization. Additionally, FK866 induces cell autophagy dependenting on de novo protein synthesis. FK866 also reduces ATP levels in ML-2 cells due to the inhibition of NAD synthesis. The antitumor efficacy of FK866 is also shown in the in vivo models. FK866 significantly prevents tumor growth both in mice xenografted subcutaneously with AML-M4 and Namalwa cells. Furthermore, FK866 clears tumor cells to below detectable levels and results in 80% survival for a long-term [1].

References:
[1] Nahimana A, Attinger A, Aubry D, Greaney P, Ireson C, Thougaard AV, Tjørnelund J, Dawson KM, Dupuis M, Duchosal MA. The NAD biosynthesis inhibitor APO866 has potent antitumor activity against hematologic malignancies. Blood. 2009 Apr 2;113(14):3276-86.

文献引用

1. Shi KL, Qian JY, et al. "Atorvastatin antagonizes the visfatin-induced expression of inflammatory mediators via the upregulation of NF-κB activation in HCAECs." Oncol Lett. 2016 Aug;12(2):1438-1444. PMID:27446449

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt391.51
Cas No.658084-64-1
FormulaC24H29N3O2
Solubility≥19.6mg/mL in DMSO, ≥49.6 mg/mL in EtOH, <2.41 mg/mL in H2O
Chemical Name(E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-pyridin-3-ylprop-2-enamide
SDFDownload SDF
Canonical SMILESC1CN(CCC1CCCCNC(=O)C=CC2=CN=CC=C2)C(=O)C3=CC=CC=C3
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

41种血液恶性肿瘤细胞系

制备方法

在DMSO中的溶解度有限。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0 ~ 10 nM;72或96小时

实验结果

在各种血液癌症细胞中,APO866 (0 ~ 10 nM) 呈剂量依赖性地诱导细胞内NAD和ATP耗竭,促进细胞死亡。

动物实验 [1]:

动物模型

人急性髓细胞白血病、淋巴瘤以及白血病细胞异种移植C.B.-17 SCID小鼠模型

给药剂量

20 mg/kg;腹腔注射;每日2次,连续四天,重复3周

实验结果

在人急性髓细胞白血病、淋巴瘤以及白血病细胞异种移植C.B.-17 SCID小鼠模型中,APO866预防并抑制肿瘤生长。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Nahimana A, Attinger A, Aubry D, Greaney P, Ireson C, Thougaard AV, Tj?rnelund J, Dawson KM, Dupuis M, Duchosal MA. The NAD biosynthesis inhibitor APO866 has potent antitumor activity against hematologic malignancies. Blood. 2009 Apr 2;113(14):3276-86.

生物活性

Description FK866是一种高特异性的和非竞争性的烟酰胺磷酸核糖转移酶(NAMPT)抑制剂,Ki值为0.4 nM。
靶点 NAMPT          
IC50 0.4 nM (Ki)          

质量控制

化学结构

FK866 (APO866)

相关生物数据

FK866 (APO866)