Daporinad (FK866)

別名：APO866

製品コード：S2799 純度：99.99%

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

CAS No. 658084-64-1

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫なし(納期7~10日)
5mg	JPY 22000	国内在庫あり
25mg	JPY 59500	国内在庫あり
50mg	JPY 100500	国内在庫あり
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（55）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Daporinad (FK866)と併用されることが多い化合物

Olaparib (AZD2281)

Daporinad and Olaparib induce double-strand DNA breaks and promote apoptosis in OV1946or cells.

Sauriol A, et al. Sci Rep. 2023 Feb 27;13(1):3334.

Niraparib (MK-4827)

Daporinad and Niraparib inhibit cell growth of olaparib-resistant cell line OV1946.

Sauriol A, et al. Sci Rep. 2023 Feb 27;13(1):3334.

KPT 9274 (ATG-019)

Daporinad and KPT 9274 are NMPT inhibitors and can strongly decrease total NAD+ levels and mitochondrial respiration in M2 macrophages.

Weinhauser I, et al. Sci Adv. 2023 Apr 14;9(15):eadf8522.

GMX1778

Daporinad and GMX1778 are iNAMPT enzymatic inhibitors that have been developed as anti-cancer treatment options.

Sun BL, et al. EBioMedicine. 2020 Nov;61:103059.

Carboplatin

Daporinad and Carboplatin combined use gives better results in inhibiting resistant cell proliferation in ovarian cancer.

Park M, et al. Front Biosci (Landmark Ed). 2023 Mar 10;28(3):47.

Daporinad (FK866)関連製品

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関連化合物ライブラリー	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	もっと見る

シグナル伝達経路

Transferaseシグナル伝達経路

Transferase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
MCF7	Antitumor assay	10 uM	6 days	Antitumor activity against human MCF7 cells at 10 uM after 6 days by SRB assay, IC50 = 0.68 μM.	21330015
MDCK	Function assay	10 uM		Apparent permeability across apical to basolateral side in dog MDCK cells at 10 uM by LC-MS/MS analysis	23859118
NYH	Cytotoxicity assay		3 weeks	Cytotoxicity against human NYH cells after 3 weeks by clonogenic survival assay, LD50 = 0.0015 μM.	23679915
A2780	Cytotoxicity assay		72 hrs	Cytotoxicity against human A2780 cells after 72 hrs by SRB assay, IC50 = 0.001 μM.	23617784
K562	Cytotoxicity assay		6 days	Cytotoxicity against human K562 cells after 6 days by SRB assay, IC50 = 20 μM.	21330015
SNU638	Cytotoxicity assay		6 days	Cytotoxicity against human SNU638 cells after 6 days by SRB assay, IC50 = 0.16 μM.	21330015
HCT116	Cytotoxicity assay		6 days	Cytotoxicity against human HCT116 cells after 6 days by SRB assay, IC50 = 0.16 μM.	21330015
A549	Cytotoxicity assay		6 days	Cytotoxicity against human A549 cells after 6 days by SRB assay, IC50 = 0.16 μM.	21330015
HT1080	Cytotoxicity assay		6 days	Cytotoxicity against human HT1080 cells after 6 days by SRB assay, IC50 = 0.16 μM.	21330015
SH-SY5Y	Cytotoxicity assay		48 hrs	Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0017 μM.	19961183
K562	Cytotoxicity assay		96 hrs	Cytotoxicity against human K562 cells after 96 hrs by MTT assay, IC50 = 0.0072 μM.	23679915
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis, IC50 = 0.001 μM.	23859118
A2780	Cytotoxicity assay		72 hrs	Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.0016 μM.	24164086
HepG2	Function assay		1 hr	Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis, IC50 = 0.0022 μM.	24164086
MCF-7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.0074 μM.	24164086
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.0109 μM.	24164086
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against APO866-resistant human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.946 μM.	24164086
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay, IC50 = 0.001 μM.	24405419
A2780	Function assay		72 hrs	Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay, IC50 = 0.001 μM.	27541271
DE3	Function assay		15 mins	Inhibition of human full length C-terminal His6-tagged NAMPT expressed in Escherichia coli Rosetta (DE3) cells using nicotinamide as substrate incubated for 15 mins prior to substrate addition measured after 30 mins in presence of PRPP, IC50 = 0.003 μM.	27541271
SH-SY5Y	Cytotoxicity assay		56 hrs	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 56 hrs by MTT assay, EC50 = 0.0034 μM.	28165742
PC3	Antiproliferative assay		5 days	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay, IC50 = 0.0057 μM.	28610984
HepG2	Cytotoxicity assay		72 hrs	Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 0.89 μM.	28885834
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.3 μM.	28885834
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.6 μM.	28885834
HepG2	Cytotoxicity assay		72 hrs	Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.89 μM.	29348808
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 1.6 μM.	29348808
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 3.7 μM.	29348808
SH-SY5Y	Autophagy assay		40 hrs	Induction of autophagy in human SH-SY5Y cells assessed as LC3/phosphotidylethanolamine coupling after 40 hrs by Western blot analysis	19961183
MCF7	Antitumor assay		6 days	Antitumor activity against human MCF7 cells after 6 days by SRB assay	21330015
MCF7	Cytotoxicity assay		96 hrs	Cytotoxicity against human MCF7 cells after 96 hrs by clonogenic assay	24164086
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay in presence of nicotinamide mononucleotide	24405419
Sf9	Function assay		30 mins	Inhibition of recombinant full length human C-terminal His/flag-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay	29348808
SH-SY5Y	Cytotoxicity assay			Cytotoxicity against human SH-SY5Y cells assessed as reduction of total cellular NAD(P) level, IC50 = 0.0005 μM.	19961183
NYH	Cytotoxicity assay			Cytotoxicity against human NYH cells by clonogenic assay, IC50 = 0.0015 μM.	24164086
PC3	Cytotoxicity assay			Cytotoxicity against human PC3 cells by clonogenic assay, IC50 = 0.0038 μM.	24164086
A2780	Cytotoxicity assay			Cytotoxicity against human A2780 cells by clonogenic assay, IC50 = 0.0057 μM.	24164086
A431	Cytotoxicity assay			Cytotoxicity against human A431 cells by clonogenic assay, IC50 = 0.0061 μM.	24164086
MCF7	Cytotoxicity assay			Cytotoxicity against human MCF7 cells by clonogenic assay, IC50 = 0.0084 μM.	24164086
SKOV3	Cytotoxicity assay			Cytotoxicity against human SKOV3 cells by clonogenic assay, IC50 = 0.211 μM.	24164086
A2780	Cytotoxicity assay			Cytotoxicity against human A2780 cells assessed as reduction in cell viability, IC50 = 0.0042 μM.	28165742
DU145	Cytotoxicity assay			Cytotoxicity against human DU145 cells by clonogenic assay	24164086
HCT116	Function assay			Resistance factor, ratio of IC50 for APO866-resistant human HCT116 cells to IC50 for human HCT116 cells	24164086
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

NMPRTase ^[5]
(Cell-free assay)

0.4 nM(Ki)

In Vitro
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]
細胞実験	細胞株	41 hematologic malignant cell lines
	濃度	0 - 10 nM
	反応時間	72 hours or 96 hours
	実験の流れ	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.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	SIRT1 p-AMPK / AMPK / p-EIF2A / EIF2A / p-4EBP1 / 4EBP1 AKT / pAKT(Ser-473) / mTOR / p-mTOR(Ser-2448)		29905535
	Immunofluorescence	pMLKL phGSK3β ph-β-catenin		29996103
	Growth inhibition assay	Cell viability		27462772

In Vivo
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]
動物実験	動物モデル	C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia.
	投与量	20 mg/kg
	投与経路	administered intraperitoneally twice a day for 4 days, repeated weekly over 3 weeks

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT00435084	Completed	B-cell Chronic Lymphocytic Leukemia	Valerio Therapeutics	February 2007	Phase 1\|Phase 2

参考
[1] Nahimana A, et al. Blood, 2009, 113(14), 3276-3286. [2] Evans L, et al. Arthritis Rheum, 2011, 63(7), 1866-1877. [3] Olesen UH, et al. Mol Cancer Ther, 2010, 9(6), 1609-1617. [4] Zoppoli G, et al. Exp Hematol, 2010, 38(11), 979-988. [5] Hasmann M, et al. Cancer Res. 2003 , 63(21):7436-42. + 展開

参考

+ 展開

化学情報

分子量	391.51	化学式	C₂₄H₂₉N₃O₂
CAS No.	658084-64-1	SDF	Download Daporinad (FK866) SDFをダウンロードする
Smiles	C1CN(CCC1CCCCNC(=O)C=CC2=CN=CC=C2)C(=O)C3=CC=CC=C3
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 78 mg/mL ( (199.22 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 78 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

よくある質問（FAQ）

質問1:
We are considering the use of S2799 for in vivo injections, Any suggestions for the formula?

回答
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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):