Daporinad (Synonyms: 达珀利奈; FK866; APO866)

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Daporinad (FK866) 是烟酰胺磷酸核糖转移酶 (NMPRTase; Nampt) 的有效抑制剂， IC₅₀ 为 0.09 nM。

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Daporinad Chemical Structure

CAS No. : 658084-64-1

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥729	In-stock
5 mg	￥663	In-stock
10 mg	￥1252	In-stock
25 mg	￥1950	In-stock
50 mg	￥2950	In-stock
100 mg	￥4400	In-stock
200 mg		询价
500 mg		询价

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Other Forms of Daporinad:

(E/Z)-Daporinad hydrochloride 询价

MCE 顾客使用本产品发表的 58 篇科研文献

: Daporinad purchased from MCE. Usage Cited in: J Cell Physiol. 2019 Apr;234(4):4385-4395. [Abstract]; SW620 and HCT116 cells are seeded into a six-well plate for 72 hr, followed by treatment with different concentrations (100 nM and 10 μM) of FK866 for 24 hr.

: Daporinad purchased from MCE. Usage Cited in: Mol Med Rep. 2017 Oct;16(4):5121-5128. [Abstract]; Effects of Emodin, FK866 and DEX on PMN apoptosis in SAP rats. Protein expression levels of Fas, FasL, Bax, cleaved caspase 3 and Bcl xL are detected by western blotting. β actin served as an internal control. Data are presented as the mean±standard deviation.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with an IC₅₀ of 0.09 nM.

IC₅₀ & Target

IC50: 0.09 nM (NMPRTase)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-431	IC₅₀	6.1 nM Compound: 1, APO866	Cytotoxicity against human A431 cells by clonogenic assay Cytotoxicity against human A431 cells by clonogenic assay	[PMID: 24164086]
A2780	IC₅₀	0.001 μM Compound: 1, APO866	Cytotoxicity against human A2780 cells after 72 hrs by SRB assay Cytotoxicity against human A2780 cells after 72 hrs by SRB assay	[PMID: 23617784]
A2780	IC₅₀	0.001 μM Compound: 2, APO-866	Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis	[PMID: 23859118]
A2780	IC₅₀	0.001 μM Compound: 2, APO-866, FK866	Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay	[PMID: 24405419]
A2780	IC₅₀	0.001 μM Compound: 8; APO866	Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay	[PMID: 27541271]
A2780	IC₅₀	0.28 nM Compound: 1; FK886	Antiproliferative activity against human A2780 cells incubated for 72 hrs in carbon-dioxide atmosphere measured by cell counting kit-8 method Antiproliferative activity against human A2780 cells incubated for 72 hrs in carbon-dioxide atmosphere measured by cell counting kit-8 method	[PMID: 36563407]
A2780	IC₅₀	1.6 nM Compound: 1, APO866	Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
A2780	IC₅₀	4.2 nM Compound: 1; FK866	Cytotoxicity against human A2780 cells assessed as reduction in cell viability Cytotoxicity against human A2780 cells assessed as reduction in cell viability	[PMID: 28165742]
A2780	IC₅₀	5.7 nM Compound: 1, APO866	Cytotoxicity against human A2780 cells by clonogenic assay Cytotoxicity against human A2780 cells by clonogenic assay	[PMID: 24164086]
A2780	IC₅₀	< 3 nM Compound: 1; FK866	Antiproliferative activity against human A2780 cells assessed as cell growth inhibition Antiproliferative activity against human A2780 cells assessed as cell growth inhibition	[PMID: 37369332]
A549	IC₅₀	0.028 μM Compound: 1; FK866; AP0866	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by cell titer glo luminescent assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by cell titer glo luminescent assay	[PMID: 35640078]
A549	IC₅₀	3.7 μM Compound: FK866	Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 29348808]
A549	IC₅₀	34.53 μM Compound: 1; FK866	Antiproliferative activity against NAMPT inhibitor-resistant A549 cells assessed as reduction in cell viability measured for 48 hrs in presence of epacadostat by CCK-8 assay Antiproliferative activity against NAMPT inhibitor-resistant A549 cells assessed as reduction in cell viability measured for 48 hrs in presence of epacadostat by CCK-8 assay	[PMID: 36595482]
A549	IC₅₀	52.15 μM Compound: 1; FK866	Antiproliferative activity against NAMPT inhibitor-resistant A549 cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay Antiproliferative activity against NAMPT inhibitor-resistant A549 cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay	[PMID: 36595482]
A549	IC₅₀	< 0.16 μM Compound: 1, FK-866	Cytotoxicity against human A549 cells after 6 days by SRB assay Cytotoxicity against human A549 cells after 6 days by SRB assay	[PMID: 21330015]
B16	IC₅₀	219 nM Compound: 1; FK866	Antitumor activity against mouse B16 cells assessed as inhibition of cell viability incubated for 72 hrs by SRB assay Antitumor activity against mouse B16 cells assessed as inhibition of cell viability incubated for 72 hrs by SRB assay	[PMID: 38060985]
BXPC-3	IC₅₀	0.3 nM Compound: 1; FK866, APO866, WK175	Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth measured after 72 hrs by XTT assay Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth measured after 72 hrs by XTT assay	[PMID: 35724566]
CT26	IC₅₀	0.039 μM Compound: FK866; AP0866	Cytotoxicity against mouse CT26 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against mouse CT26 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38722799]
CT26	IC₅₀	34.9 nM Compound: 1; FK866	Antitumor activity against mouse CT26 cells assessed as inhibition of cell viability incubated for 72 hrs by SRB assay Antitumor activity against mouse CT26 cells assessed as inhibition of cell viability incubated for 72 hrs by SRB assay	[PMID: 38060985]
DU-145	IC₅₀	5.12 nM Compound: FK866, APO866; 1	Antiproliferative activity against human DU145 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human DU145 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
HCCLM3	IC₅₀	0.4 μM Compound: FK866	Antiproliferative activity against human HCCLM3 cells incubated for 120 hrs in presence of JQ1 by MTT assay Antiproliferative activity against human HCCLM3 cells incubated for 120 hrs in presence of JQ1 by MTT assay	[PMID: 38691889]
HCCLM3	IC₅₀	1.01 μM Compound: FK866	Antiproliferative activity against human HCCLM3 cells incubated for 120 hrs by MTT assay Antiproliferative activity against human HCCLM3 cells incubated for 120 hrs by MTT assay	[PMID: 38691889]
HCT-116	IC₅₀	1.6 μM Compound: 2; FK228	Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28885834]
HCT-116	IC₅₀	1.6 μM Compound: FK866	Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 29348808]
HCT-116	IC₅₀	10.9 nM Compound: 1, APO866	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
HCT-116	IC₅₀	946 nM Compound: 1, APO866	Cytotoxicity against APO866-resistant human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against APO866-resistant human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
HCT-116	IC₅₀	< 0.16 μM Compound: 1, FK-866	Cytotoxicity against human HCT116 cells after 6 days by SRB assay Cytotoxicity against human HCT116 cells after 6 days by SRB assay	[PMID: 21330015]
HL-60	GI₅₀	12.1 nM Compound: FK866	Antiproliferative activity against p53-null human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based fluorescence analysis Antiproliferative activity against p53-null human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based fluorescence analysis	[PMID: 38224650]
HT-1080	IC₅₀	< 0.16 μM Compound: 1, FK-866	Cytotoxicity against human HT1080 cells after 6 days by SRB assay Cytotoxicity against human HT1080 cells after 6 days by SRB assay	[PMID: 21330015]
HUVEC	IC₅₀	< 0.001 nM Compound: 1; FK866	Cytotoxicity activity against HUVEC cells assessed as cell growth inhibition Cytotoxicity activity against HUVEC cells assessed as cell growth inhibition	[PMID: 37369332]
HeLa	GI₅₀	1.34 nM Compound: 1; APO-866; FK866	Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay	[PMID: 27224875]
HeLa	IC₅₀	3.75 nM Compound: FK866, APO866; 1	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
Hep 3B2	IC₅₀	1.55 μM Compound: FK866	Synergistic antiproliferative activity against human Hep3B cells measured after 72 hrs in presence of JQ1 Synergistic antiproliferative activity against human Hep3B cells measured after 72 hrs in presence of JQ1	[PMID: 38691889]
Hep 3B2	IC₅₀	53.67 μM Compound: FK866	Antiproliferative activity against human Hep3B cells incubated for 120 hrs by MTT assay Antiproliferative activity against human Hep3B cells incubated for 120 hrs by MTT assay	[PMID: 38691889]
Hep 3B2	IC₅₀	53.67 μM Compound: FK866	Antiproliferative activity against human Hep3B cells measured after 72 hrs Antiproliferative activity against human Hep3B cells measured after 72 hrs	[PMID: 38691889]
HepG2	IC₅₀	0.89 μM Compound: 2; FK228	Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28885834]
HepG2	IC₅₀	0.89 μM Compound: FK866	Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 29348808]
HepG2	IC₅₀	18.72 nM Compound: 1; FK866	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay	[PMID: 31818629]
HepG2	IC₅₀	2.2 nM Compound: 1, APO866	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 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	[PMID: 24164086]
Huh-7	IC₅₀	0.67 μM Compound: FK866	Antiproliferative activity against human Huh-7 cells incubated for 120 hrs in presence of JQ1 by MTT assay Antiproliferative activity against human Huh-7 cells incubated for 120 hrs in presence of JQ1 by MTT assay	[PMID: 38691889]
Huh-7	IC₅₀	1.05 nM Compound: FK866, APO866; 1	Antiproliferative activity against human HuH7 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human HuH7 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
Huh-7	IC₅₀	2.12 μM Compound: FK866	Antiproliferative activity against human Huh-7 cells incubated for 120 hrs by MTT assay Antiproliferative activity against human Huh-7 cells incubated for 120 hrs by MTT assay	[PMID: 38691889]
Jurkat	IC₅₀	0.6 nM Compound: 1; FK866, APO866, WK175	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by XTT assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by XTT assay	[PMID: 35724566]
Jurkat	IC₅₀	0.73 nM Compound: 1; FK866, APO866	Cytotoxicity against human Jurkat cells assessed as inhibition of cell viability at 72 hrs by SRB assay Cytotoxicity against human Jurkat cells assessed as inhibition of cell viability at 72 hrs by SRB assay	[PMID: 36787658]
K562	IC₅₀	0.96 nM Compound: FK866, APO866; 1	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
K562	IC₅₀	7.2 nM Compound: 1, FK866, WK175, APO866	Cytotoxicity against human K562 cells after 96 hrs by MTT assay Cytotoxicity against human K562 cells after 96 hrs by MTT assay	[PMID: 23679915]
K562	IC₅₀	> 20 μM Compound: 1, FK-866	Cytotoxicity against human K562 cells after 6 days by SRB assay Cytotoxicity against human K562 cells after 6 days by SRB assay	[PMID: 21330015]
LN-18	IC₅₀	33.6 nM Compound: 1; FK866	Antitumor activity against human LN-18 cells assessed as inhibition of cell viability incubated for 72 hrs by SRB assay Antitumor activity against human LN-18 cells assessed as inhibition of cell viability incubated for 72 hrs by SRB assay	[PMID: 38060985]
LX-2	IC₅₀	0.21 μM Compound: FK866	Antiproliferative activity against human LX2 cells incubated for 120 hrs by MTT assay Antiproliferative activity against human LX2 cells incubated for 120 hrs by MTT assay	[PMID: 38691889]
LX-2	IC₅₀	< 0.032 μM Compound: FK866	Antiproliferative activity against human LX2 cells incubated for 120 hrs in presence of JQ1 by MTT assay Antiproliferative activity against human LX2 cells incubated for 120 hrs in presence of JQ1 by MTT assay	[PMID: 38691889]
MCF7	GI₅₀	0.29 nM Compound: 1; APO-866; FK866	Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay	[PMID: 27224875]
MCF7	IC₅₀	0.41 nM Compound: FK866, APO866; 1	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
MCF7	IC₅₀	0.68 μM Compound: 1, FK-866	Antitumor activity against human MCF7 cells at 10 uM after 6 days by SRB assay Antitumor activity against human MCF7 cells at 10 uM after 6 days by SRB assay	[PMID: 21330015]
MCF7	IC₅₀	7.4 nM Compound: 1, APO866	Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
MCF7	IC₅₀	8.4 nM Compound: 1, APO866	Cytotoxicity against human MCF7 cells by clonogenic assay Cytotoxicity against human MCF7 cells by clonogenic assay	[PMID: 24164086]
MDA-MB-231	GI₅₀	0.78 nM Compound: 1; APO-866; FK866	Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay	[PMID: 27224875]
MDA-MB-231	IC₅₀	1.3 μM Compound: 2; FK228	Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28885834]
MIA PaCa-2	IC₅₀	0.34 nM Compound: 1; FK866, APO866	Antitumor activity in human MIA PaCa-2 cells assessed as intracellular NAD+ depletion incubated for 24 hrs by enzymatic cycling assay Antitumor activity in human MIA PaCa-2 cells assessed as intracellular NAD+ depletion incubated for 24 hrs by enzymatic cycling assay	[PMID: 36787658]
MIA PaCa-2	IC₅₀	2.2 nM Compound: 1; FK866, APO866, WK175	Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth measured after 72 hrs by XTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth measured after 72 hrs by XTT assay	[PMID: 35724566]
MIA PaCa-2	IC₅₀	2.4 nM Compound: 1; FK866, APO866	Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell viability at 72 hrs by SRB assay Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell viability at 72 hrs by SRB assay	[PMID: 36787658]
ML-2	IC₅₀	0.24 nM Compound: 1; FK866, APO866	Cytotoxicity against human ML-2 cells assessed as inhibition of cell viability at 72 hrs by SRB assay Cytotoxicity against human ML-2 cells assessed as inhibition of cell viability at 72 hrs by SRB assay	[PMID: 36787658]
MV4-11	GI₅₀	7.95 nM Compound: FK866	Antiproliferative activity against human MV4-11 cells harboring wild type p53 assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based fluorescence analysis Antiproliferative activity against human MV4-11 cells harboring wild type p53 assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based fluorescence analysis	[PMID: 38224650]
MV4-11	IC₅₀	15.3 nM Compound: FK866	Antiproliferative activity against human MV4-11 cells harboring wild type p53 assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based fluorescence analysis Antiproliferative activity against human MV4-11 cells harboring wild type p53 assessed as inhibition of cell growth incubated for 48 hrs by resazurin dye based fluorescence analysis	[PMID: 38224650]
NAMALVA	IC₅₀	0.37 nM Compound: 1; FK866, APO866	Cytotoxicity against human NAMALVA cells assessed as inhibition of cell viability at 72 hrs by SRB assay Cytotoxicity against human NAMALVA cells assessed as inhibition of cell viability at 72 hrs by SRB assay	[PMID: 36787658]
NB-4	IC₅₀	2 nM Compound: 1; FK866, APO866	Cytotoxicity against human NB4 cells assessed as inhibition of cell viability at 72 hrs by SRB assay Cytotoxicity against human NB4 cells assessed as inhibition of cell viability at 72 hrs by SRB assay	[PMID: 36787658]
NCI-H1975	GI₅₀	3.95 nM Compound: 1; APO-866; FK866	Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay	[PMID: 27224875]
NCI-H1975	IC₅₀	4.76 nM Compound: FK866, APO866; 1	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutation assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutation assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
PANC-1	IC₅₀	0.6 nM Compound: 1; FK866, APO866, WK175	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth measured after 72 hrs by XTT assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth measured after 72 hrs by XTT assay	[PMID: 35724566]
PC-3	IC₅₀	0.006 μM Compound: 4; FK866	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by Celltiter-Glo assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by Celltiter-Glo assay	[PMID: 31303996]
PC-3	IC₅₀	3.8 nM Compound: 1, APO866	Cytotoxicity against human PC3 cells by clonogenic assay Cytotoxicity against human PC3 cells by clonogenic assay	[PMID: 24164086]
PC-3	IC₅₀	5.7 nM Compound: 1; FK866	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay	[PMID: 28610984]
RPMI-8226	IC₅₀	0.76 nM Compound: 1; FK866, APO866	Cytotoxicity against human RPMI-8226 cells assessed as inhibition of cell viability at 72 hrs by SRB assay Cytotoxicity against human RPMI-8226 cells assessed as inhibition of cell viability at 72 hrs by SRB assay	[PMID: 36787658]
SH-SY5Y	EC₅₀	2.5 nM Compound: 4; FK866	Cytotoxicity against human SH-SY5Y cells measured after 48 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells measured after 48 hrs by MTT assay	[PMID: 31400709]
SH-SY5Y	EC₅₀	3.2 nM Compound: FK866	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00261C
SH-SY5Y	EC₅₀	3.4 nM Compound: 1; FK866	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 56 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 56 hrs by MTT assay	[PMID: 28165742]
SH-SY5Y	IC₅₀	0.5 nM Compound: 1, FK-866, APO-866	Cytotoxicity against human SH-SY5Y cells assessed as reduction of total cellular NAD(P) level Cytotoxicity against human SH-SY5Y cells assessed as reduction of total cellular NAD(P) level	[PMID: 19961183]
SH-SY5Y	IC₅₀	1.7 nM Compound: 1, FK-866, APO-866	Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 19961183]
SH-SY5Y	IC₅₀	30.1 pM Compound: FK866	Inhibition of NAMPT in human SH-SY5Y cells assessed as NAD depletion incubated for 16 hrs Inhibition of NAMPT in human SH-SY5Y cells assessed as NAD depletion incubated for 16 hrs	10.1039/C5MD00261C
SK-OV-3	IC₅₀	0.006 μM Compound: FK866; AP0866	Cytotoxicity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38722799]
SK-OV-3	IC₅₀	211 nM Compound: 1, APO866	Cytotoxicity against human SKOV3 cells by clonogenic assay Cytotoxicity against human SKOV3 cells by clonogenic assay	[PMID: 24164086]
SNU-638	IC₅₀	< 0.16 μM Compound: 1, FK-866	Cytotoxicity against human SNU638 cells after 6 days by SRB assay Cytotoxicity against human SNU638 cells after 6 days by SRB assay	[PMID: 21330015]
U-87MG ATCC	IC₅₀	0.41 μM Compound: 7; FK866	Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	0.45 μM Compound: 7; FK866	Synergistic antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs in presence of IDH305 by CCK8 assay Synergistic antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs in presence of IDH305 by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	0.56 μM Compound: 7; FK866	Synergistic antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs in presence of AG-120 by CCK8 assay Synergistic antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs in presence of AG-120 by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	0.97 μM Compound: 7; FK866	Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	1.04 μM Compound: 7; FK866	Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	1.63 μM Compound: 7; FK866	Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	1.69 μM Compound: 7; FK866	Synergistic antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs in presence of IDH305 by CCK8 assay Synergistic antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs in presence of IDH305 by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	2.51 μM Compound: 7; FK866	Synergistic antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs in presence of AG-120 by CCK8 assay Synergistic antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs in presence of AG-120 by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	2.55 μM Compound: 7; FK866	Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	5.46 μM Compound: 7; FK866	Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay	[PMID: 38651495]
U-937	GI₅₀	0.36 nM Compound: 1; APO-866; FK866	Cytotoxicity against human U937 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against human U937 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay	[PMID: 27224875]

体外研究
(In Vitro)

使用 (E)-Daporinad 抑制 Nampt 可诱导细胞内 NAD⁺ 显著减少并选择性杀死 MM 细胞。(E)-Daporinad 诱导的细胞死亡与 Nampt 活性抑制有关，而非蛋白质表达，并且 MM 细胞中 NAD⁺ 基线水平高于正常 PBMC，这赋予了 (E)-Daporinad 敏感性。 (E)-Daporinad 消除了骨髓微环境赋予的生存优势^[1]。 (E)-Daporinad 可防止不同丝裂原诱导的 [Ca²⁺]i 升高，并降低 Jurkat 和活化的 PBL 中 TG 反应性 Ca²⁺ 库的 Ca²⁺ 含量。(E)-Daporinad 可降低 Jurkat 细胞中 TG 反应性 Ca²⁺ 库的 Ca²⁺ 含量，但不会降低 Bcl2-Jurkat 细胞中的 TG 反应性 Ca²⁺ 含量^[2]。 (E)-Daporinad 抑制 NAMPT 或烟酰胺抑制 SIRT 可降低涉及 p53 乙酰化途径的 293T 细胞增殖并引发其死亡^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

(E)-Daporinad (FK866) (30 mg/kg，腹腔注射) 降低 CB17-SCID 小鼠的肿瘤负担，肿瘤组织中 ERK 磷酸化和 LC3^[1] 蛋白水解酶裂解显著减少。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

391.51

Formula

C₂₄H₂₉N₃O₂

CAS 号

658084-64-1

性状

固体

颜色

White to light yellow

中文名称

达珀利奈

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 50 mg/mL (127.71 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5542 mL	12.7711 mL	25.5421 mL
5 mM	0.5108 mL	2.5542 mL	5.1084 mL
10 mM	0.2554 mL	1.2771 mL	2.5542 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.39 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.39 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.39 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 50% PEG300 50% Saline
Solubility: 5 mg/mL (12.77 mM); 澄清溶液; 超声助溶
方案二

请依序添加每种溶剂： 20% SBE-β-CD in Saline
Solubility: 4 mg/mL (10.22 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.91%

选择批次：

Data Sheet (642 KB) SDS (393 KB)

COA (280 KB) HNMR (223 KB) LCMS (402 KB) 元素分析报告 (204 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Cea M, et al. Targeting NAD+ salvage pathway induces autophagy in multiple myeloma cells via mTORC1 and extracellular signal-regulated kinase (ERK1/2) inhibition. Blood. 2012 Oct 25;120(17):3519-29. [Content Brief]

[2]. Magnone M, et al. NAD+ levels control Ca2+ store replenishment and mitogen-induced increase of cytosolic Ca2+ by Cyclic ADP-ribose-dependent TRPM2 channel gating in human T lymphocytes. J Biol Chem. 2012 Jun 15;287(25):21067-81. [Content Brief]

[3]. Thakur BK, et al. Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells. Biochem Biophys Res Commun. 2012 Aug 3;424(3):371-7. [Content Brief]

Cell Assay ^[1]	MM1S cells (2×10⁴ cells/well) are cultured for 72 and 96 hours in BMSC-coated 96-well plates in the presence or absence of drug. DNA synthesis is measured by (³H)-thymidine uptake, with (³H)-thymidine added (0.5 μCi/well) during the last 8 hours of cultures. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	CB17-SCID mice (28-35 days old) are irradiated (200 cGy), and then inoculated subcutaneously in the right flank with 3×10⁶ MM1S cells in 100 μL RPMI 1640. After detection of tumor (2 weeks after the injection), 7 mice are treated intraperitoneally with either vehicle or (E)-Daporinad (FK866) (30 mg/kg body weight) twice a day for 4 days, repeated weekly over 3 weeks. Caliper measurements of the longest perpendicular tumor diameters are performed twice a week to estimate the tumor volume using the following formula: length×width²×0.5. Tumor growth inhibition (TGI) is calculated. Animals are killed when tumors reach 2 cm³ or the mice appear moribund. Survival is evaluated from the first day of treatment until death. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Cea M, et al. Targeting NAD+ salvage pathway induces autophagy in multiple myeloma cells via mTORC1 and extracellular signal-regulated kinase (ERK1/2) inhibition. Blood. 2012 Oct 25;120(17):3519-29. [Content Brief] [2]. Magnone M, et al. NAD+ levels control Ca2+ store replenishment and mitogen-induced increase of cytosolic Ca2+ by Cyclic ADP-ribose-dependent TRPM2 channel gating in human T lymphocytes. J Biol Chem. 2012 Jun 15;287(25):21067-81. [Content Brief] [3]. Thakur BK, et al. Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells. Biochem Biophys Res Commun. 2012 Aug 3;424(3):371-7. [Content Brief]

Daporinad 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5542 mL	12.7711 mL	25.5421 mL	63.8553 mL
	5 mM	0.5108 mL	2.5542 mL	5.1084 mL	12.7711 mL
	10 mM	0.2554 mL	1.2771 mL	2.5542 mL	6.3855 mL
	15 mM	0.1703 mL	0.8514 mL	1.7028 mL	4.2570 mL
	20 mM	0.1277 mL	0.6386 mL	1.2771 mL	3.1928 mL
	25 mM	0.1022 mL	0.5108 mL	1.0217 mL	2.5542 mL
	30 mM	0.0851 mL	0.4257 mL	0.8514 mL	2.1285 mL
	40 mM	0.0639 mL	0.3193 mL	0.6386 mL	1.5964 mL
	50 mM	0.0511 mL	0.2554 mL	0.5108 mL	1.2771 mL
	60 mM	0.0426 mL	0.2129 mL	0.4257 mL	1.0643 mL
	80 mM	0.0319 mL	0.1596 mL	0.3193 mL	0.7982 mL
	100 mM	0.0255 mL	0.1277 mL	0.2554 mL	0.6386 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Daporinad (Synonyms: 达珀利奈; FK866; APO866)

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MCE 顾客使用本产品发表的 58 篇科研文献

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Daporinad (Synonyms: 达珀利奈; FK866; APO866)

Customer Review

Other Forms of Daporinad:

Daporinad 相关抗体

MCE 顾客使用本产品发表的 58 篇科研文献

Daporinad 相关产品

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