FK866 (APO866)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
FK866是烟酰胺磷酸核糖转移酶(NMPRTase)的抑制剂,IC50值介于0.09-27.2 nM之间[1]。
NAD在许多生化和生物学过程中起至关重要的作用。与正常细胞相比,癌细胞有更高的NAD成交率,因此,靶向NAD的合成被认识是一种选择性杀死癌细胞的方式。
在MTT实验中,41个人类血癌细胞系均对低浓度的FK866敏感,其中AML细胞是最敏感的。FK866对人类血液恶性肿瘤细胞具有选择性,而正常人HPCs对FK866具有抗性。FK866以caspase不依赖的方式诱导细胞死亡,但以剂量依赖的方式诱导线粒体膜去极化。此外,FK866诱导细胞自噬,依赖于从头蛋白质的合成。在ML-2细胞中,FK866通过抑制NAD的合成,从而减少ATP水平[1]。
FK866的抗肿瘤效应在体内模型中显示。在皮下异种移植AML-M4或Namalwa细胞的小鼠中,FK866显著抑制肿瘤的生长。而且,FK866清除肿瘤细胞至低于可检测的水平,导致80%小鼠的长期存活[1]。
参考文献:
[1] Nahimana A, Attinger A, Aubry D, Greaney P, Ireson C, Thougaard AV, Tjrnelund 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.
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Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 391.51 |
Cas No. | 658084-64-1 |
Formula | C24H29N3O2 |
Solubility | insoluble in H2O; ≥19.6 mg/mL in DMSO; ≥49.6 mg/mL in EtOH |
Chemical Name | (E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-pyridin-3-ylprop-2-enamide |
SDF | Download SDF |
Canonical SMILES | C1CN(CCC1CCCCNC(=O)C=CC2=CN=CC=C2)C(=O)C3=CC=CC=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
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) |
质量控制和MSDS
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