Daporinad (FK866, APO866)

Catalog No.S2799

Molecular Weight(MW): 391.51

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

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Bar graph showing the effect of the PBEF inhibitor FK866 on PLB-induced autophagy in PC-3 cells. Data are presented as the mean ± SD of three independent experiments. *P<0.05; **P<0.01; and ***P<0.001 by one-way ANOVA.

Drug Des Devel Ther, 2015, 9: 1511-54. Daporinad (FK866, APO866) purchased from Selleck.

Paraffin-embedded tumor sections derived from MiaPaCa-2 were stained with H&E or anti-Ki67 antibodies (Scale bar: 100 μm); apoptotic cells were visualized by TUNEL staining (green) and counterstained with DAPI (blue) (Scale bar: 10 μm). The proliferation index and apoptotic index in tumor sections were also quantified. These animal experiments were repeated once (n = 5mice per treatment group).

Cancer Lett, 2016, 379(1):1-11.. Daporinad (FK866, APO866) purchased from Selleck.
Effect of metabolic inhibitors on SRC-1 protein levels. A549 cells grown in glucose-containing medium were treated with NAM or FK866 at the indicated concentration.

Mol Endocrinol 2014 28(3), 395-405. Daporinad (FK866, APO866) purchased from Selleck.

Purity & Quality Control

Choose Selective Transferase Inhibitors

Biological Activity

Description

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

Targets

NMPRTase ^[5]
(Cell-free assay)

0.4 nM(Ki)

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]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
human SH-SY5Y cells	NFfBSHZEgXSxdH;4bYPDqGG\|c3H5			MoLhR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2guW1l3WTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhfG:2YXygZ4VtdHWuYYKgUmFFMFBrIHzleoVtNCCLQ{WwQVAvPSCwTR?=	M{TBcFE6QTZzMUiz
human A2780 cells	M4fjVHBzd2yrZnXyZZRqd25iYYPzZZk>		NEfzdZk4OiCq	M2ey[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEmFNUC9NUBvVQ>?	MYOyOFQxPTRzOR?=
human NYH cells	MmrzR5l1d3SxeHnjxsBie3OjeR?=		M4DPWVMhf2Wna4O=	MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOXWgh[2WubIOgZYZ1\XJiMzD3[YVseyCkeTDjcI9vd2enbnnjJJN2en[rdnHsJIF{e2G7LDDJR\|UxRTFwNTDuUS=>	MkDxNlM3Pzl7MUW=
human HepG2 cells	MWDGeY5kfGmxbjDhd5NigQ>?		MYixJIg>	NYO5fYdkUW6qaXLpeIlwdiCxZjDORW1RXCCrbjDoeY1idiCKZYDHNkBk\WyuczD1d4lv\yCdMUTDYU1vcWOxdHnuZY1q\GVxUGLQVEBieyC\|dXLzeJJifGViYYPz[ZN{\WRiYYOg[o9zdWG2aX;uJI9nKFtzNFPdMY5q[2:2aX7hcYll\SCvb37vcpVkdGWxdHnk[UBi\nSncjCxJIhzKGK7IHzpdZVq\CC\|Y3nueIltdGG2aX;uJINwfW62aX7nJIFv[Wy7c3nzMEBKSzVyPUKuNkBvVQ>?	MWOyOFE3PDB6Nh?=
human PC3 cells	NHjEOW9EgXSxdH;4bYPDqGG\|c3H5			NUfkT2NoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN\|IHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVA:Oy56IH7N	M1XmSlI1OTZ2MEi2
human A431 cells	NVjoRoJJS3m2b4TvfIlkyqCjc4PhfS=>			MkTFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVYvOSCwTR?=	M3HqdVI1OTZ2MEi2
human K562 cells	NVrlcIw2S3m2b4TvfIlkyqCjc4PhfS=>		Mo\rPVYhcA>?	NHnYUVJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZktKEmFNUC9O{4zKG6P	NXeyUVhlOjN4N{m5NVU>
human MCF-7 cells	NGXDNHhEgXSxdH;4bYPDqGG\|c3H5		M371N\|czKGh?	MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2YuPyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVA:Py52IH7N	M{TjeFI1OTZ2MEi2
human HCT116 cells	Mn\xR5l1d3SxeHnjxsBie3OjeR?=		NY\xSHgzPzJiaB?=	MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO\|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR\|UxRTFyLkmgcm0>	MVeyOFE3PDB6Nh?=
human HT1080 cells	NFjvSIhEgXSxdH;4bYPDqGG\|c3H5		MnXMOkBl[Xm\|	MV3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWFExQDBiY3XscJMh[W[2ZYKgOkBl[Xm\|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlE3KM7:TR?=	NHPjcHczOTN\|MECxOS=>
human HCT116 cells	NGnzNZBEgXSxdH;4bYPDqGG\|c3H5		NEfkfYk3KGSjeYO=	M1TRemN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA3KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOTZizszN	NIPNdnQzOTN\|MECxOS=>
human A549 cells	NY\EZ5hvS3m2b4TvfIlkyqCjc4PhfS=>		M1uwS\|Yh\GG7cx?=	NEjvS5VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUC9NE4yPiEQvF2=	M1rBfVIyOzNyMEG1
human SNU638 cells	NG\uVlZEgXSxdH;4bYPDqGG\|c3H5		MXq2JIRigXN?	M{LkfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNPXTZ\|ODDj[YxteyCjZoTldkA3KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOTZizszN	MVuyNVM{ODBzNR?=
human SKOV3 cells	NYPZSWR4S3m2b4TvfIlkyqCjc4PhfS=>			MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVIyOSCwTR?=	M{DjelI1OTZ2MEi2
human MCF7 cells	MlnTSpVv[3Srb36gZZN{[Xl?	MlfJNVAh\|ryP	MmPGOkBl[Xm\|	NFK3TmxCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIF1KDFyIIXNJIFnfGW{IE[g[IF6eyCkeTDTVmIh[XO\|YYmsJGlEPTB;MD62PEDPxE1?	M2\OSFIyOzNyMEG1

... Click to View More Cell Line Experimental Data

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]

Protocol

Cell Research: ^[1]	+ Expand 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. (Only for Reference)
Animal Research: ^[1]	+ Expand 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 (Only for Reference)

Cell Research:

^[1]

+ Expand

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.

(Only for Reference)

Animal Research:

^[1]

+ Expand

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
(Only for Reference)

References

+ Expand

Solubility (25°C)

In vitro	Ethanol	78 mg/mL (199.22 mM)
	DMSO	Insoluble
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 45% Propylene glycol (dissolve first)+5% Tween 80+ddH2O For best results, use promptly after mixing.	15mg/mL

* 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 Information Download Daporinad (FK866, APO866) SDF

Molecular Weight	391.51
Formula	C₂₄H₂₉N₃O₂
CAS No.	658084-64-1
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-11-16)

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

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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.

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Frequently Asked Questions

Question 1:
We are considering the use of S2799 for in vivo injections, Any suggestions for the formula?
Answer:
The vehicle we recommend for S2799 in vivo study is 45% Propylene glycol (dissolve first) +5% Tween 80+ddH2O. You can dissolve the compound in Propylene glycol first and then dilute with water with Tween 80. The solution is clear and can be used for injection.

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Daporinad (FK866, APO866)