Cat. No.: HY-50876

Daporinad

(Synonyms: FK866; APO866)

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Daporinad (FK866) is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a K_i value of 0.3 nM. Daporinad depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad causes the depletion of the endoplasmic reticulum Ca²⁺ pool, ultimately weakening the mitogen-induced Ca²⁺ signal and the activation and function of T cells. Daporinad induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad can be used for the study of myeloma, liver cancer, and immunosuppression.

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Pureté: 99.91%
CAS No.: 658084-64-1
Formule: C₂₄H₂₉N₃O₂
Masse moléculaire:391.51

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

Daporinad Chemical Structure

CAS No.: 658084-64-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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Description

IC₅₀ & Target

IC50: 0.09 nM (NMPRTase)

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Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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]
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]
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]
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	<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]
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]
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]
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]
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]
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]
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	>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]
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]
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	<0.032 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]
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]
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]

In Vitro

Nampt inhibition with (E)-Daporinad (FK866) induces significant NAD⁺ intracellular reduction and selectively kills MM cells. (E)-Daporinad (FK866)-induced cell death is associated with inhibition of Nampt activity, rather than protein expression, and higher NAD⁺ baseline levels in MM cells than normal PBMCs confer (E)-Daporinad (FK866) sensitivity. (E)-Daporinad (FK866) abrogates the survival advantage conferred by the bone marrow microenvironment^[1]. (E)-Daporinad (FK866) prevents the [Ca²⁺]i increase induced by different mitogens and reduces the Ca²⁺ content of TG-responsive Ca²⁺ stores in Jurkat and in activated PBLs. (E)-Daporinad (FK866) reduces the Ca²⁺ content of TG-responsive Ca²⁺ stores in Jurkat cells but not in Bcl2-Jurkat cells^[2]. Inhibition of NAMPT by (E)-Daporinad (FK866), or inhibition of SIRT by nicotinamide decreases proliferation and triggered death of 293T cells involving the p53 acetylation pathway^[3].

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

In Vivo

Daporinad (FK866) (30 mg/kg, i.p.) decreases the tumor burden in CB17-SCID mice, and the tumor tissue demonstrates a significant decrease in ERK phosphorylation and proteolytic cleavage of LC3^[1].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 658084-64-1
Appearance Solid
Masse moléculaire 391.51
Formule C₂₄H₂₉N₃O₂
Color White to light yellow
SMILES

O=C(C1=CC=CC=C1)N(CC2)CCC2CCCCNC(/C=C/C3=CC=CN=C3)=O
Synonyms

FK866; APO866
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (67)

All Flow CytometryHistological Imaging/StainingWB

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Journal Impact Factor

Cell Metab

Nicotinamide metabolism face-off between macrophages and fibroblasts manipulates the microenvironment in gastric cancer. [Abstract]

2024 Jun 18:S1550-4131(24)00189-X. PMID: 38897198

Daporinad purchased from MedChemExpress. Usage Cited in: Cell Metab. 2024 Jun 18:S1550-4131(24)00189-X. [Abstract]

Flow cytometry analysis of M1 (CD86) and M2 (CD206) markers in human peripheral blood-derived macrophages or NAMPT-overexpressing (oxNAMPT) macrophages both treated with FK866 (10 nM, 48 h).
Nat Commun

Nuclear IMPDH2 controls the DNA damage response by modulating PARP1 activity. [Abstract]

2024 Nov 12;15(1):9515. PMID: 39532854
Cell Death Differ

TREM2 macrophage promotes cardiac repair in myocardial infarction by reprogramming metabolism via SLC25A53. [Abstract]

2024 Feb;31(2):239-253. PMID: 38182899
Adv Sci (Weinh)

Unraveling the Microenvironment and the Pathogenic Axis of HIF-1α-Visfatin-Fibrosis in Autoimmune Pancreatitis Using a Single-Cell Atlas. [Abstract]

2025 Jan 31:e2412282. PMID: 39887620
J Adv Res

Single-Cell RNA sequencing identifies NAMPT as a potential therapeutic target in autoimmune uveitis. [Abstract]

2025 Dec 29:S2090-1232(25)01020-3. PMID: 41475661

Daporinad purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Dec 29:S2090-1232(25)01020-3. [Abstract]

Representative ocular fundus images and clinical scores from the Normal, EAU, and NAMPTi (FK866; 10 mg/kg; ip; daily for 14 days ) groups at day 14 post-immunization. White arrows highlight inflammatory infiltrates and vascular abnormalities. B. Representative histopathological images and histological scores from the Normal, EAU and NAMPTi groups at day 14 post-immunization. Black arrows highlight inflammatory cell infiltration, retinal detachment, and retinal folding.

Daporinad purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Dec 29:S2090-1232(25)01020-3. [Abstract]

NAMPT inhibition ameliorates EAU by modulating the Teff/Treg balance and suppressing Hif1a in CD4+ T cells in vivo. A-B. Frequencies of CD4⁺IL 17A⁺ (Th17) cells and CD4⁺ IFN γ⁺(Th1) cells in both CDLNs (A) and spleen (B) of EAU and NAMPTi (FK866; 10 mg/kg; ip; daily for 14 days ) treated EAU mice on day 14 post-immunization. C-D. Frequencies of CD4⁺-CD25⁺Foxp3⁺ (Treg) cells in both CDLNs (C) and spleen (D).
Exp Mol Med

CD300E+ macrophages facilitate liver regeneration after splenectomy in decompensated cirrhotic patients. [Abstract]

2025 Feb;57(1):72-85. PMID: 39741181
Sci Adv

A dual chemodrug-loaded hyaluronan nanogel for differentiation induction therapy of refractory AML via disrupting lysosomal homeostasis. [Abstract]

2025 Mar 28;11(13):eado3923. PMID: 40153509
Sci Adv

M2 macrophages drive leukemic transformation by imposing resistance to phagocytosis and improving mitochondrial metabolism. [Abstract]

2023 Apr 14;9(15):eadf8522. PMID: 37058562
Redox Biol

SIRT1 activated by AROS sensitizes glioma cells to ferroptosis via induction of NAD+ depletion-dependent activation of ATF3. [Abstract]

2024 Feb:69:103030. PMID: 38181705
Cell Death Dis

Targeting metabolic vulnerability by combining NAMPT inhibitors and disulfiram for treatment of recurrent ovarian cancer. [Abstract]

2025 Apr 25;16(1):342. PMID: 40280967
Acta Pharmacol Sin

Activated SIRT1 contributes to DPT-induced glioma cell parthanatos by upregulation of NOX2 and NAT10. [Abstract]

2023 Oct;44(10):2125-2138. PMID: 37277492
Acta Pharmacol Sin

TAX1BP1 contributes to deoxypodophyllotoxin-induced glioma cell parthanatos via inducing nuclear translocation of AIF by activation of mitochondrial respiratory chain complex I. [Abstract]

2023 Sep;44(9):1906-1919. PMID: 37186123
Cell Chem Biol

AspSnFR: A genetically encoded biosensor for real-time monitoring of aspartate in live cells. [Abstract]

2024 May 20:S2451-9456(24)00179-X. PMID: 38806058
Sci Signal

Metabolic perturbations sensitize triple-negative breast cancers to apoptosis induced by BH3 mimetics. [Abstract]

2021 Jun 8;14(686):eabc7405. PMID: 34103421
J Agric Food Chem

Palmatine Attenuated Lipopolysaccharide-Induced Acute Lung Injury by Inhibiting M1 Phenotype Macrophage Polarization via NAMPT/TLR2/CCR1 Signaling. [Abstract]

2024 Apr 15. PMID: 38619332
JCI Insight

A shift in PKM2 oligomeric state instructs adipocyte inflammatory potential. [Abstract]

2025 Nov 24;10(22):e185914. PMID: 41277555
Chem Biol Interact

Melatonin suppresses glycolysis and coordinately disrupts DNA repair via targeting the YAP1-NAMPT signaling in breast cancer. [Abstract]

2026 Feb 11:425:111900. PMID: 41485639
Cells

NAD+ Acts as a Protective Factor in Cellular Stress Response to DNA Alkylating Agents. [Abstract]

2023 Oct 2;12(19):2396. PMID: 37830610
Commun Biol

Nicotinamide mononucleotide treatment improves spermatogenesis in obese mice by reducing lysine acetylation of lactate dehydrogenase C. [Abstract]

2025 Nov 26;8(1):1761. PMID: 41298813
PLoS Pathog

Nicotinamide metabolism is essential for Hepatitis C Virus replication and the production of infectious Lipo-Viro-Particles. [Abstract]

2026 Apr 22;22(4):e1014165. PMID: 42018568
Biol Direct

NAMPT modulates muscle fiber type transition in PAD myopathy via the cGMP-PKG signaling pathway. [Abstract]

2025 Nov 27;20(1):113. PMID: 41310770
PLoS Pathog

Resident bacteria contribute to opportunistic infections of the respiratory tract. [Abstract]

2021 Mar 19;17(3):e1009436. PMID: 33740012
Front Pharmacol

Trimetazidine Inhibits Renal Tubular Epithelial Cells to Mesenchymal Transition in Diabetic Rats via Upregulation of Sirt1. [Abstract]

2020 Jul 29;11:1136. PMID: 32848753
Eur J Pharm Sci

Activation of nicotinamide phosphoribosyltransferase protects against unilateral renal ischemia-reperfusion injury via the NAD+/SIRT1/PGC-1α signaling pathway and modulation of NFκB/TNF-α/IL-6. [Abstract]

2025 Sep 29:214:107302. PMID: 41033563
Int Immunopharmacol

Cisatracurium besylate rescues Mycobacterium Tuberculosis-infected macrophages from necroptosis and enhances the bactericidal effect of isoniazid. [Abstract]

2023 Jul:120:110291. PMID: 37182451
Biol Res

NAMPT regulates mitochondria and oxidative stress level for mouse early embryo development. [Abstract]

2025 May 4;58(1):25. PMID: 40320561
Molecules

Quantitative Analysis of Daporinad (FK866) and Its In Vitro and In Vivo Metabolite Identification Using Liquid Chromatography-Quadrupole-Time-of-Flight Mass Spectrometry. [Abstract]

2022 Mar 21;27(6):2011. PMID: 35335372
Clin Epigenetics

Investigating the mechanisms by which low NAT1 expression in tumor cells contributes to chemo-resistance in colorectal cancer. [Abstract]

2025 May 6;17(1):77. PMID: 40329330
Cancers (Basel)

High-Dosage NMN Promotes Ferroptosis to Suppress Lung Adenocarcinoma Growth through the NAM-Mediated SIRT1-AMPK-ACC Pathway. [Abstract]

2023 Apr 23;15(9):2427. PMID: 37173894
Front Cell Dev Biol

AZD5153, a Bivalent BRD4 Inhibitor, Suppresses Hepatocarcinogenesis by Altering BRD4 Chromosomal Landscape and Modulating the Transcriptome of HCC Cells. [Abstract]

2022 Mar 24:10:853652. PMID: 35399501
Mol Neurobiol

The Depletion of NAMPT Disturbs Mitochondrial Homeostasis and Causes Neuronal Degeneration in Mouse Hippocampus. [Abstract]

2023 Mar;60(3):1267-1280. PMID: 36441480
Biochim Biophys Acta Mol Basis Dis

Chlorophyllides repress gain-of-function p53 mutated HNSCC cell proliferation via activation of p73 and repression of p53 aggregation in vitro and in vivo. [Abstract]

2025 Jan 7:167662. PMID: 39788216
Biochim Biophys Acta Mol Basis Dis

Effect of alternating nicotinamide phosphoribosyltransferase expression levels on mitophagy in Alzheimer's disease mouse models. [Abstract]

2024 Jun 9:167288. PMID: 38862096
J Inflamm Res

Decrease of NAD+ Inhibits the Apoptosis of OLP T Cells via Inducing Mitochondrial Fission. [Abstract]

2025 Jan 23:18:1091-1106. PMID: 39871961
Adv Photonics Res

2026 Apr 18;7(4):e202500258.
J Cell Physiol

NAMPT regulates mitochondria function and lipid metabolism during porcine oocyte maturation. [Abstract]

2024 Jan;239(1):180-192. PMID: 37992208
J Cell Physiol

Nicotinamide phosphoribosyl transferase regulates cell growth via the Sirt1/P53 signaling pathway and is a prognosis marker in colorectal cancer. [Abstract]

2019 Apr;234(4):4385-4395. PMID: 30191976

Daporinad purchased from MedChemExpress. 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.
Sci Rep

Inhibition of nicotinamide dinucleotide salvage pathway counters acquired and intrinsic poly(ADP-ribose) polymerase inhibitor resistance in high-grade serous ovarian cancer. [Abstract]

2023 Feb 27;13(1):3334. PMID: 36849518
J Biol Chem

Glucose-6-phosphate dehydrogenase exerts anti-stress effects independently of its enzymatic activity. [Abstract]

2022 Dec;298(12):102587. PMID: 36243112
Brain Res Bull

Ablation of NAMPT in dopaminergic neurons leads to neurodegeneration and induces Parkinson's disease in mouse. [Abstract]

2024 Nov 1:218:111114. PMID: 39489186
Clin Exp Med

SPOP-dependent destabilization of SYT12 in a GSK-3β-dependent manner in papillary thyroid cancer cells. [Abstract]

2025 Jul 10;25(1):243. PMID: 40640517
Mol Med Rep

Emodin alleviates severe acute pancreatitis-associated acute lung injury by decreasing pre-B-cell colony-enhancing factor expression and promoting polymorphonuclear neutrophil apoptosis. [Abstract]

2017 Oct;16(4):5121-5128. PMID: 28849044

Daporinad purchased from MedChemExpress. 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.
Mol Carcinog

Adipocytes Promote Endometrial Cancer Progression Through Activation of the SIRT1-HMMR Signaling Axis. [Abstract]

2024 Dec;63(12):2363-2381. PMID: 39254492
Pancreatology

Inhibition of nicotinamide phosphoribosyltransferase protects against acute pancreatitis via modulating macrophage polarization and its related metabolites. [Abstract]

2021 Aug;21(5):870-883. PMID: 33810973
Cancer Manag Res

Is the Fixed Periodic Treatment Effective for the Tumor System without Complete Information?. [Abstract]

2021 Nov 30;13:8915-8928. PMID: 34876854
PeerJ

Oxidative stress induces cell death partially by decreasing both mRNA and protein levels of nicotinamide phosphoribosyltransferase in differentiated PC12 cells. [Abstract]

2021 May 14;9:e11401. PMID: 34040894
Neurosci Lett

Inhibition of neuronal Kv7 channels ameliorates MK-801-induced cognitive dysfunction in mice via up-regulating NAMPT expression. [Abstract]

2023 Sep 25:814:137471. PMID: 37673371
Genes Genomics

FK866 inhibits colorectal cancer metastasis by reducing NAD+ levels in cancer-associated fibroblasts. [Abstract]

2022 Dec;44(12):1531-1541. PMID: 36214983
Rapid Commun Mass Spectrom

Daporinad in vitro metabolite profiling via rat, dog, monkey and human liver microsomes by liquid chromatography/quadrupole-orbitrap mass spectrometry. [Abstract]

2021 Sep 30;35(18):e9150. PMID: 34159659
bioRxiv

2026 May 21.
Res Sq

2026 Mar 5.
bioRxiv

2025 Dec 25.
bioRxiv

2025 Oct 14.
Res Sq

2025 Sep 23.
bioRxiv

2025 Aug 02.
bioRxiv

A Novel FNDC1-NAMPT-NAD axis is Implicated in Small and Large-vessel Arterial Disease and Drives Vascular Calcification. [Abstract]

2025 Jul 10:2025.07.08.663801. PMID: 40672352
Res Sq

Novel mixed cancer-cell models designed to capture inter-patient tumor heterogeneity for accurate evaluation of drug combinations. [Abstract]

2025 May 16:rs.3.rs-6590535. PMID: 40470249
bioRxiv

2025 March 26.
bioRxiv

PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]

2024 Nov 6:2024.11.04.621884. PMID: 39574568
University of Minnesota

2024.
Research Square Preprint

2024 Apr 12.
Research Square Preprint

2024 Mar 6.
Research Square Preprint

2023 Nov 14.
Research Square Preprint

2023 Sep 8.
bioRxiv

2019 Oct.
bioRxiv

2019 Oct 28.
Patent

US20180263995A1.

Solvant et solubilité

In Vitro:

DMSO : ≥ 50 mg/mL (127.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 5 mg/mL (12.77 mM); Clear solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 20% SBE-β-CD in Saline

Solubility: 4 mg/mL (10.22 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

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.

MedChemExpress (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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
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Références

[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]

[4]. Hasmann M, Schemainda I. FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis. Cancer Res. 2003 Nov 1;63(21):7436-42. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	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

Keywords

Daporinad

67 Cited Publications

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Daporinad

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Metabolism/Protease Compound Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

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Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

RNA Binding Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Daporinad

Voir tous les produits spécifiques à Isoform mTOR

Voir tous les produits spécifiques à Isoform p38 MAPK

Voir tous les produits spécifiques à Isoform ERK

Activité biologique

Chemical Information

Publications (67)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Daporinad Related Classifications

HY-50876 Related Classifications