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CAS No.: 658084-64-1

(E)-Daporinad/达珀利奈 Catalog No. CSN16330

Synonyms: FK866;APO866;Daporinad

FK866 effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay.

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生物活性

实验方案

技术信息

生物活性

描述Nicotinamide phosphoribosyltransferase (NAPRT) is a key enzyme in the regulation of NAD+ biosynthesis from the natural precursor nicotinamide. FK866 (Daporinad, APO866) effectively inhibited NAPRT with IC50 value of 0.09nM in a cell-free assay, which not directly inhibited mitochondrial respiratory activity, but caused gradual NAD+ depletion through specific inhibition of NAPRT. FK866 may be used for treatment of diseases implicating deregulated apoptosis such as cancer or as a sensitizer for genotoxic agents. At low concentrations ranging from 0.09-27nM, FK866 induced dose-dependent cytotoxicity in 41 hematologic malignant cells including acute myeloid leukemia, acute lymphoblastic leukemia, T-cell lymphoma and so on. While at concentrations from 0-10nM, FK866 induced cell death independent on caspase activation associated with depolarization of mitochondrial membrane. FK866 at concentrations ranging in 0-10nM also induced depletion of intracellular NAD and ATP contents and cell death in various hematologic cancer cells. Treatment with 10nM FK866 in mice with CIA, synovial inflammation was inhibited, including chemokine-directed leukocyte infiltration and serum hyaluronic acid. Besides, expression of MMP-3 and MMP-13 in joint extracts was reduced and also to a reduction in a systemic marker of cartilage erosion, serum cartilage oligomeric matrix protein. PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells was reduced. FK866 was investigated in 24 patients with advanced cancers in a phase I study aiming to determine the dose-limiting toxicity (DLT) and maximum tolerated dose (MTD). At dose levels higher than 0.036 mg/m2/hr CTC grade III lymphocytopenia not thought to be clinically relevant, preceded all other toxicities. The recommended dose for phase II studies is 0.126 mg/m2/hr administered by civ infusion for 4 consecutive days every 4 weeks.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human A2780 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay, IC50=1 nM	24405419
human A431 cells	-	Cytotoxic assay	-	Cytotoxicity against human A431 cells by clonogenic assay, IC50=6.1 nM	24164086
human A549 cells	-	Cytotoxic assay	6 days	Cytotoxicity against human A549 cells after 6 days by SRB assay, IC50=0.16 μM	21330015

更多
动物研究
剂量
Rat: 0.5 mg/kg^[3] (i.p.) Mice: 30 mg/kg^[4] (i.p.), 100 mg/kg^[5] (i.p.)

给药途径
i.p.

动物研究
剂量	Rat: 0.5 mg/kg^[3] (i.p.) Mice: 30 mg/kg^[4] (i.p.), 100 mg/kg^[5] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5542 mL
- 12.7712 mL
- 25.5424 mL
- 5 mM
- 0.5108 mL
- 2.5542 mL
- 5.1085 mL
- 10 mM
- 0.2554 mL
- 1.2771 mL
- 2.5542 mL

技术信息

CAS号

658084-64-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H29N3O2

运输

蓝冰

分子量

391.51

别名

FK866;APO866;Daporinad;K 22.175;达珀利奈

溶解度

DMSO	110.0 mg/mL (281.0 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	2 mg/mL	clear
PO	0.5% CMC-Na	30 mg/mL	suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

human A2780 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay, IC50=1 nM	24405419
human A431 cells	-	Cytotoxic assay	-	Cytotoxicity against human A431 cells by clonogenic assay, IC50=6.1 nM	24164086
human A549 cells	-	Cytotoxic assay	6 days	Cytotoxicity against human A549 cells after 6 days by SRB assay, IC50=0.16 μM	21330015
human HCT116 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50=10.9 nM	24164086
human HCT116 cells	-	Cytotoxic assay	6 days	Cytotoxicity against human HCT116 cells after 6 days by SRB assay, IC50=0.16 μM	21330015
human HepG2 cells	-	Function assay	1 h	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=2.2 nM	24164086
human HT1080 cells	-	Cytotoxic assay	6 days	Cytotoxicity against human HT1080 cells after 6 days by SRB assay, IC50=0.16 μM	21330015
human K562 cells	-	Cytotoxic assay	96 h	Cytotoxicity against human K562 cells after 96 hrs by MTT assay, IC50=7.2 nM	23679915
human MCF7 cells	10 μM	Function assay	6 days	Antitumor activity against human MCF7 cells at 10 uM after 6 days by SRB assay, IC50=0.68 μM	21330015
human MCF-7 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50=7.4 nM	24164086
human NYH cells	-	Cytotoxic assay	3 weeks	Cytotoxicity against human NYH cells after 3 weeks by clonogenic survival assay, IC50=1.5 nM	23679915
human PC3 cells	-	Cytotoxic assay	-	Cytotoxicity against human PC3 cells by clonogenic assay, IC50=3.8 nM	24164086
human SH-SY5Y cells	-	Cytotoxic assay	-	Cytotoxicity against human SH-SY5Y cells assessed as reduction of total cellular NAD(P) level, IC50=0.5 nM	19961183
human SKOV3 cells	-	Cytotoxic assay	-	Cytotoxicity against human SKOV3 cells by clonogenic assay, IC50=211 nM	24164086
human SNU638 cells	-	Cytotoxic assay	6 days	Cytotoxicity against human SNU638 cells after 6 days by SRB assay, IC50=0.16 μM	21330015

(E)-Daporinad/达珀利奈 Catalog No. CSN16330

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