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FK866(APO866,Daporinad)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FK866(APO866,Daporinad)图片
CAS NO:658084-64-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)391.51
FormulaC24H29N3O2
CAS No.658084-64-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 78 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)45% Propylene glycol (dissolve first)+5% Tween 80+ddH2O: 15mg/mL
SynonymsAPO 866; FK 866; FK-866; Daporinad; APO866; APO-866; FK866; K 22.175;
实验参考方法
In Vitro

In vitro activity: APO866 at low concentrations ranging from 0.09-27 nM induces dose-dependent cytotoxicity in 41 hematologic malignant cells including acute myeloid leukemia [AML], acute lymphoblastic leukemia [ALL], mantle cell lymphoma [MCL], chronic lymphocytic leukemia [CLL], and T-cell lymphoma. APO866 at low concentrations ranging from 0-10 nM induces cell death, this effect is independent of caspase activation but is associated with depolarization of mitochondrial membrane. APO866 at concentrations ranging from 0-10 nM dose-dependently induces depletion of intracellular NAD and ATP contents and cell death in various hematologic cancer cells. APO866 at concentration of 10 nM inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells.


Cell Assay: For MTT assays, 0.5 × 106 cells/mL is plated in triplicate on 96-well plates. APO866 (0.01 nM-100 nM) is added in 50 μL of culture medium, with culture medium alone serving as control. After 72 or 96 hours of incubation, 15 μL of dye solution is added to each well and cells are incubated for an additional 4 hours. Stop solution (100 μL/well) is added for 1 hour and the absorbance is read at 570 nm on a spectrophotometer. For trypan blue dye exclusion staining, 0.5 × 105 cells/well is grown in 6-well plates with 1 mL media in the absence or presence of APO866 for 96 hours. Cells from each sample are incubated with 10 μL trypan blue solution (at a 1:1 ratio [vol/vol] for 1 minute). Cell survival is determined by calculating proportion of live (unstained) cells.

In VivoAPO866 administered intraperitoneally at dose of 20 mg/kg twice a day for 4 days, repeat weekly over 3 weeks, prevents and abrogats tumor growth in C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia. APO866 at dose of 0.12 mg/kg/hour prevents joint destruction and leukocyte infiltration through inhibition of PBEF in mice with CIA.
Animal modelC.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia.
Formulation & DosageDissolved in 0.9% saline; 20 mg/kg; i.p. injection
References

Blood. 2009 Apr 2;113(14):3276-86; Arthritis Rheum. 2011 Jul;63(7):1866-77.