Daporinad (Synonyms: FK866; APO866)

Name: Daporinad
Brand: MedChemExpress
SKU: HY-50876
Rating: 5.0 (64 reviews)

Cat. No.: HY-50876 Purity: 99.91%: Data Sheet
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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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CAS No. : 658084-64-1

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무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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고객리뷰

Based on 64 publication(s) in Google Scholar

Other Forms of Daporinad:

(E/Z)-Daporinad hydrochloride 견적 받기
Daporinad hydrochloride 견적 받기

64 Publications Citing Use of MCE Daporinad

Flow Cytometry

Histological Imaging/Staining

: 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).

: 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).

: 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.

: 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.

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Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

IC50: 0.09 nM (NMPRTase)

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]

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.

Clinical Trial

분자량

391.51

화학식

C₂₄H₂₉N₃O₂

CAS No.

658084-64-1

Appearance

Solid

Color

White to light yellow

SMILES

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* 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.

몰농도 계산기
농도 희석 계산기

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.

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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.91%

Select Batch:

Data Sheet (276 KB) SDS (396 KB)

COA (243 KB) HNMR (268 KB) LCMS (95 KB) Elemental Analysis Report (101 KB)

Handling Instructions (2659 KB)

References

[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]

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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
References	[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]

Complete Stock Solution Preparation Table

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

Daporinad Related Classifications

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: FK866; APO866)

고객리뷰

Other Forms of Daporinad:

64 Publications Citing Use of MCE Daporinad

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References

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몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Daporinad Related Classifications

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Daporinad (Synonyms: FK866; APO866)

고객리뷰

Other Forms of Daporinad:

Daporinad Related Antibodies

64 Publications Citing Use of MCE Daporinad

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All mTOR Isoform Specific Products:

View All p38 MAPK Isoform Specific Products:

View All ERK Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

Daporinad Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Daporinad Related Classifications

Keywords:

최근 본 상품:

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SAFETY DATA SHEET (SDS)

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