Daporinad (FK866)

别名: APO866 中文名称：达珀利奈

目录号：S2799 Purity: 99.99%

Daporinad (FK866)有效抑制烟酰胺磷酸核糖转移酶(NMPRTase; Nampt)，Daporinad (FK866) 可引发自噬，无细胞试验中IC50为0.09 nM。Phase 1/2。

Daporinad (FK866) Chemical Structure

CAS: 658084-64-1

规格	价格	库存
10mM (1mL in DMSO)	1613.43	现货
5mg	737.65	现货
10mg	1405.61	现货
25mg	3025.95	现货
50mg	4662.84	现货
1g	24488.1	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

产品质控

批次：纯度： 99.99%

99.99

常与Daporinad (FK866)一起在实验中被使用的化合物

Olaparib (AZD2281)

Daporinad和Olaparib诱导双链DNA断裂并促进OV1946or细胞凋亡。

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

Niraparib (MK-4827)

Daporinad和Niraparib抑制olaparib耐药细胞系OV1946的细胞生长。

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

KPT 9274 (ATG-019)

Daporinad和KPT9274是NMPT抑制剂，可以强烈降低M2巨噬细胞中的总NAD+水平和线粒体呼吸。

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

GMX1778

Daporinad和GMX1778是iNAMPT酶抑制剂，已被开发为抗癌治疗选择。

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

Carboplatin

Daporinad和Carboplatin联合使用在抑制卵巢癌耐药细胞增殖方面具有更好的效果。

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

Daporinad (FK866)相关产品

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相关化合物库	代谢化合物库抗癌代谢化合物库谷氨酰胺代谢化合物库糖代谢化合物库脂代谢化合物库	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
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
点击查看更多细胞系数据

生物活性

产品描述

Daporinad (FK866)有效抑制烟酰胺磷酸核糖转移酶(NMPRTase; Nampt)，Daporinad (FK866) 可引发自噬，无细胞试验中IC50为0.09 nM。Phase 1/2。

靶点

NMPRTase ^[5]
(Cell-free assay)

0.4 nM(Ki)

体外研究(In Vitro)
体外研究活性	APO866在0.09-27 nM的低浓度范围内会在41血液恶性肿瘤细胞中诱导产生细胞毒性，包括急性髓细胞白血病[AML]，急性淋巴细胞白血病 [ALL], 套细胞淋巴瘤[MCL], 慢性淋巴细胞白血病[CLL]和 T细胞淋巴瘤，这种毒性具有剂量依赖特性. APO866在0-10 nM的低浓度范围内会诱导细胞死亡，这一效果与线粒体膜去极化有关而与半胱天冬酶的激活无关。APO866在0-10 nM的浓度范围内会诱导胞内NAD 和 ATP 的损耗和多种血液肿瘤细胞的死亡，这一效果具有剂量依赖特性^[1] 。10 nM APO866 会抑制HFFF2细胞内 PBEF诱导的 MMP-3, CCL2和CXCL8 的分泌 ^[2]。
细胞实验	细胞系	41血液恶性肿瘤细胞系
	浓度	0 - 10 nM
	孵育时间	72 小时或 96小时
	方法	MTT 分析流程, 细胞按每毫升0.5 &time 10⁶ 个的密度接种到96孔板，接种三份。将APO866 (0.01 nM-100 nM) 加到50 μL 培养基中, 空白培养基作为对照。孵育 72或 96 小时后每孔加入15 μL 染料溶液继续孵育 4 小时。然后每孔加入100 μL 终止液孵育 1小时，用分光光度计测量570 nm 处吸光度。台盼蓝染色分析流程, 细胞按每孔0.5 &time10⁵ 个接种到6孔板，每孔加入1 mL培养基，在含有或缺少 APO866的情况下孵育 96 小时。每孔取10μL 细胞样品与10 μL 台盼蓝孵育1分钟（体积比1:1）。细胞存活情况通过计算未染色的细胞个数来获得。
实验图片	检测方法	检测指标	实验图片	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

体内研究(In Vivo)
体内研究活性	用C.B.-17 SCID 小鼠建立人急性髓细胞白血病，淋巴母细胞淋巴瘤和白血病的异种移植模型，腹腔注射APO866 ，一天两次，一次20 mg/kg 一周4天, 重复三周以上可以抑制肿瘤生长。 ^[1]对于携带CIA的小鼠， 0.12 mg/kg/小时剂量的 APO866 可以通过抑制PBEF 来防止关节破坏和白细胞浸润^[2]。
动物实验	Animal Models	人急性髓细胞白血病，淋巴瘤以及白血病的C.B.-17 SCID 小鼠异种移植模型
	Dosages	20 mg/kg
	Administration	腹腔注射一天两次，连续四天，重复3周以上

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00435084	Completed	B-cell Chronic Lymphocytic Leukemia	Valerio Therapeutics	February 2007	Phase 1\|Phase 2

参考文献
[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. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	391.51	分子式	C₂₄H₂₉N₃O₂
CAS号	658084-64-1	SDF	Download Daporinad (FK866) SDF
Smiles	C1CN(CCC1CCCCNC(=O)C=CC2=CN=CC=C2)C(=O)C3=CC=CC=C3
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 78 mg/mL ( (199.22 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 78 mg/mL (199.22 mM)

Water : Insoluble

DMSO : 78 mg/mL ( (199.22 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 78 mg/mL (199.22 mM)

Water : Insoluble

DMSO : 80 mg/mL ( (204.33 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 78 mg/mL (199.22 mM)

Water : Insoluble

DMSO : 78 mg/mL ( (199.22 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 78 mg/mL (199.22 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解配方批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂				动物体内配方计算器
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	4.000mg/ml (10.22mM)	以 1 mL 工作液为例，取50μL80mg/ml的澄清DMSO储备液加到400μL PEG300中，混合均匀使其澄清；向上述体系中加入50μLTween80，混合均匀使其澄清；然后继续加入500μL ddH2O定容至 1 mL。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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操作手册

如果有其他问题，请给我们留言。

* 必填项

常见问题及建议解决方法

问题 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):

Daporinad (FK866)

产品质控

常与Daporinad (FK866)一起在实验中被使用的化合物

Daporinad (FK866)相关产品

相关信号通路图

细胞实验数据示例

生物活性

化学信息&溶解度

实验计算

技术支持

常见问题及建议解决方法