FK866 (APO866, Daporinad)

Catalog No.S2799

FK866 (APO866, Daporinad) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. Phase 1/2.

Price Stock Quantity  
USD 90 In stock
USD 170 In stock
USD 370 In stock
USD 570 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

FK866 (APO866, Daporinad) Chemical Structure

FK866 (APO866, Daporinad) Chemical Structure
Molecular Weight: 391.51

Validation & Quality Control

3 customer reviews :

Quality Control & MSDS

Related Compound Libraries

FK866 (APO866, Daporinad) is available in the following compound libraries:

Product Information

  • Compare Transferase Inhibitors
    Compare Transferase Products
  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description FK866 (APO866, Daporinad) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. Phase 1/2.
Targets NMPRTase [1]
(Cell-free assay)
IC50 0.09 nM
In vitro 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. [1] APO866 at concentration of 10 nM inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells. [2]
In vivo APO866 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. [1] APO866 at dose of 0.12 mg/kg/hour prevents joint destruction and leukocyte infiltration through inhibition of PBEF in mice with CIA. [2]
Features

Protocol(Only for Reference)

Cell Assay:

[1]

Cell lines 41 hematologic malignant cell lines
Concentrations 0 - 10 nM
Incubation Time 72 hours or 96 hours
Method

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.

Animal Study:

[1]

Animal Models C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia.
Formulation 0.9% saline
Dosages 20 mg/kg
Administration administered intraperitoneally twice a day for 4 days, repeated weekly over 3 weeks

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Nahimana A, et al. Blood, 2009, 113(14), 3276-3286.

[2] Evans L, et al. Arthritis Rheum, 2011, 63(7), 1866-1877.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT00431912 Completed Cutaneous T-cell Lymphoma Onxeo February 2007 Phase 2
NCT00435084 Completed B-cell Chronic Lymphocytic Leukemia Onxeo February 2007 Phase 1|Phase 2
NCT00432107 Completed Melanoma Onxeo July 2006 Phase 2

Chemical Information

Download FK866 (APO866, Daporinad) SDF
Molecular Weight (MW) 391.51
Formula

C24H29N3O2

CAS No. 658084-64-1
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro Ethanol 78 mg/mL (199.22 mM)
DMSO <1 mg/mL
Water <1 mg/mL
In vivo 45% Propylene glycol (dissolve first)+5% Tween 80+ddH2O 15mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name (E)-N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Transferase Products

Recently Viewed Items

Tags: buy FK866 (APO866, Daporinad) | FK866 (APO866, Daporinad) supplier | purchase FK866 (APO866, Daporinad) | FK866 (APO866, Daporinad) cost | FK866 (APO866, Daporinad) manufacturer | order FK866 (APO866, Daporinad) | FK866 (APO866, Daporinad) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us