Daporinad (FK866, APO866)

Name: Daporinad (FK866, APO866)
Brand: Selleck Chemicals
SKU: S2799
Rating: 5 (25 reviews)

For research use only.

Catalog No.S2799

25 publications

Daporinad (FK866, APO866) Chemical Structure

Molecular Weight(MW): 391.51

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

Selleck's Daporinad (FK866, APO866) has been cited by 25 publications

Cell Metab, 2020, 31(3):564-579

PubMed: 32130883 ( click the link to review the publication )

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Nat Biotechnol, 2017, 35(5):463-474

PubMed: 28319085 ( click the link to review the publication )

Cancer Discov, 2016, 6(7):727-39

PubMed: 27231123 ( click the link to review the publication )

Mol Ther Nucleic Acids, 2020, 1;20:801-811

PubMed: 32438315 ( click the link to review the publication )

Front Cell Dev Biol, 2020, 17;8:191

PubMed: 32363189 ( click the link to review the publication )

Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669

PubMed: 32238439 ( click the link to review the publication )

Cell Microbiol, 2020, 22(1):e13115

PubMed: 31509891 ( click the link to review the publication )

Toxicol In Vitro, 2020, 65:104808

PubMed: 32087266 ( click the link to review the publication )

Cell Commun Signal, 2020, 18(1):16

PubMed: 32005247 ( click the link to review the publication )

Leukemia, 2020, 10.1038/s41375-019-0692-5

PubMed: 31896781 ( click the link to review the publication )

Nat Commun, 2019, 10(1):3790

PubMed: 31439867 ( click the link to review the publication )

Cancers (Basel), 2019, 11(12)

PubMed: 31795447 ( click the link to review the publication )

J Cell Physiol, 2019, 10.1002/jcp.28910

PubMed: 31141164 ( click the link to review the publication )

Mol Psychiatry, 2018, 10.1038/s41380-018-0061-1

PubMed: 29728703 ( click the link to review the publication )

Nat Commun, 2018, 9(1):502

PubMed: 29402884 ( click the link to review the publication )

Cell chemical biology, 2018, 10.1016/j.chembiol.2017.12.008

PubMed: 29307841 ( click the link to review the publication )

Cell Physiol Biochem, 2018, 49(6):2463-2482

PubMed: 30261504 ( click the link to review the publication )

J Cell Physiol, 2018, 233(9):7402-7414

PubMed: 29663373 ( click the link to review the publication )

Neural Plast, 2017, 2017:7019803

PubMed: 28656112 ( click the link to review the publication )

Cancer Lett, 2016, 379(1):1-11

PubMed: 27233476 ( click the link to review the publication )

Drug Des Devel Ther, 2015, 9:1555-84

PubMed: 25792811 ( click the link to review the publication )

Drug Des Devel Ther, 2015, 10.2147/DDDT.S75976

PubMed: ( click the link to review the publication )
Mol Endocrinol, 2014, 28(3):395-405

PubMed: 24438340 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Transferase Inhibitors

Biological Activity

Description

Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) 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	NV\rWGV[S3m2b4TvfIlkyqCjc4PhfS=>			NH36SHNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iC2b4ThcEBk\WyudXzhdkBPSURqUDmgcIV3\WxuIFnDOVA:OC53IH7N	M1O3dVE6QTZzMUiz
human A2780 cells	MXXQdo9tcW[ncnH0bY9vKGG\|c3H5		NEfpU404OiCq	MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGy\|IHHmeIVzKDd{IHjyd{BjgSC\|dXzmc5Jpd2SjbXnu[UBDKGG\|c3H5MEBKSzVyPUGgcm0>	MWKyOFQxPTRzOR?=
human NYH cells	M2PTXWN6fG:2b4jpZ:Kh[XO\|YYm=		NIDsSYQ{KHenZXvz	M1GyOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5[UCClZXzsd{Bi\nSncjCzJJdm\Wu\|IHL5JINtd26xZ3XubYMhe3W{dnn2ZYwh[XO\|YYmsJGlEPTB;MT61JI5O	NInIWY4zOzZ5OUmxOS=>
human HepG2 cells	MmDHSpVv[3Srb36gZZN{[Xl?		MVixJIg>	MlP2TY5pcWKrdHnvckBw\iCQQV3QWEBqdiCqdX3hckBJ\XCJMjDj[YxteyC3c3nu[{BcOTSFXT3ubYNwfGmwYX3p[IUwWFKSUDDhd{B{fWK\|dILheIUh[XO\|ZYPz[YQh[XNiZn;ycYF1cW:wIH;mJHsyPEOfLX7pZ491cW6jbXnk[UBud26xboXjcIVwfGmmZTDh[pRmeiBzIHjyJIJ6KGyrcYXp[EB{[2mwdHnscIF1cW:wIHPveY51cW6pIHHuZYx6e2m\|LDDJR\|UxRTJwMjDuUS=>	NWXSRoN[OjRzNkSwPFY>
human PC3 cells	MXzDfZRwfG:6aXRCpIF{e2G7			MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR\|Mh[2WubIOgZpkh[2yxbn;n[Y5q[yCjc4PhfUwhUUN3ME2zMlghdk1?	MoHiNlQyPjRyOE[=
human A431 cells	NGLETo5EgXSxdH;4bYPDqGG\|c3H5			NI\nUYpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVA:Pi5zIH7N	NFy2VXUzPDF4NEC4Oi=>
human K562 cells	M1zrO2N6fG:2b4jpZ:Kh[XO\|YYm=		NGHYTYc6PiCq	NHnHPXZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZktKEmFNUC9O{4zKG6P	NWm1c5hCOjN4N{m5NVU>
human MCF-7 cells	MmrQR5l1d3SxeHnjxsBie3OjeR?=		M4PTdFczKGh?	NV;uSpRPS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOILUegZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGfTWE0yKGG\|c3H5MEBKSzVyPUeuOEBvVQ>?	Mnv1NlQyPjRyOE[=
human HCT116 cells	NHza[GpEgXSxdH;4bYPDqGG\|c3H5		NEfCV3c4OiCq	M17aOGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliV2PUMVEh[XO\|YYmsJGlEPTB;MUCuPUBvVQ>?	NETycG8zPDF4NEC4Oi=>
human HT1080 cells	NVn6OHNzS3m2b4TvfIlkyqCjc4PhfS=>		NHnuW5g3KGSjeYO=	NXzCe5ZPS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRzMEiwJINmdGy\|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVA:OC5zNjFOwG0>	MmrCNlE{OzByMUW=
human HCT116 cells	NWnIWoo{S3m2b4TvfIlkyqCjc4PhfS=>		MX:2JIRigXN?	MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOkBl[Xm\|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlE3KM7:TR?=	Ml[3NlE{OzByMUW=
human A549 cells	MUfDfZRwfG:6aXRCpIF{e2G7		NUCyXFEzPiCmYYnz	NGDVRZJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUC9NE4yPiEQvF2=	MlvONlE{OzByMUW=
human SNU638 cells	M2W5XmN6fG:2b4jpZ:Kh[XO\|YYm=		M3znOlYh\GG7cx?=	Ml\XR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV25WPjN6IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUC9NE4yPiEQvF2=	MkTrNlE{OzByMUW=
human SKOV3 cells	NFXCZWxEgXSxdH;4bYPDqGG\|c3H5			MoDzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NF0zOTFibl2=	NXLBRoVbOjRzNkSwPFY>
human MCF7 cells	NXHjdoVYTnWwY4Tpc44h[XO\|YYm=	MlLPNVAh\|ryP	MkPHOkBl[Xm\|	Mn;iRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDheEAyOCC3TTDh[pRmeiB4IHThfZMh[nliU2LCJIF{e2G7LDDJR\|UxRTBwNkig{txO	MkTQNlE{OzByMUW=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	SIRT1; PubMed: 29905535 Aging (Albany NY) Human retinal pigment epithelial cells (ARPE-19) were treated with different doses (0.01-10μM) of FK866 and expression of SIRT1 was evaluated by western blotting. p-AMPK / AMPK / p-EIF2A / EIF2A / p-4EBP1 / 4EBP1; PubMed: 29541451 Cancer Metab CEM PA cells were treated with 5 and 100 nM FK866 for 48 h. Western blot showing expression of AMPK, mTOR, 4EBP1, and EIF2A in CEM PA cells. AKT / pAKT(Ser-473) / mTOR / p-mTOR(Ser-2448); PubMed: 26542945 BMC Cancer Jurkat cells were treated for 48 h with or without (Mock) the indicated concentration of FK866. Thereafter, cells were lysed and the levels of total and p-Akt (Ser-473), total and p-MTOR (Ser-2448), total and p-4EBP1 (Ser-65 and Thr-70).	29905535 29541451 26542945
Immunofluorescence	pMLKL; PubMed: 29996103 Cell Rep Immunofluorescence for pMLKL (monoclonal pMLKL antibody, red, phospho S358) and nuclei (DAPI, blue) in THP-1 cells treated with the indicated concentrations of FK866 for 6 hr. Scale bars, 10 μm. phGSK3β; PubMed: 22207684 Haematologica Representative DUOLINK images of phospho-GSK3β (Ser9) protein expression in HL60 cells treated with 10 nM of FK866 for 96 h or 100 nM of AC93253 for 48 h, or with DMSO as a control. ph-β-catenin ; PubMed: 22207684 Haematologica Representative images of inactive phospho-β-catenin (Ser33/37) protein expression in HL60 cells treated with 10 nM of FK866, 100 nM of AC93253 or DMSO as a control	29996103 22207684
Growth inhibition assay	Cell viability ; PubMed: 27462772 Oncotarget Twenty-three PDAC-derived PCCs were treated for 72 h with increasing concentrations of FK866 ranging from 0 to 1000 nM. The horizontal dotted line indicates 50% cell viability. PCCs with the highest sensitivity are highlighted by a blue line and those wit䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ	27462772

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]

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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]

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

References

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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): 5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O For best results, use promptly after mixing.	4mg/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
Smiles	O=C(NCCCCC1CCN(CC1)C(=O)C2=CC=CC=C2)/C=C/C3=CC=CN=C3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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)