FK866; APO866 MedChemExpress (MCE)

Product Name	FK866 (APO866, Daporinad)
Synonyms	FK 866 APO-866 K 22.175 FK866 (APO866) FK866 (APO866, Daporinad) (E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE (2E)-N-[4-(1-Benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2-propenamide Synonyms FK 866 APO-866 K 22.175 FK866 (APO866) FK866 (APO866, Daporinad) (E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE (2E)-N-[4-(1-Benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2-propenamide 2-PROPENAMIDE, N-[4-(1-BENZOYL-4-PIPERIDINYL)BUTYL]-3-(3-PYRIDINYL)-, (2E)-
CAS	658084-64-1
EINECS
Chemical Formula	C24H29N3O2
Molecular Weight	391.51
inchi
Package	10 mM * 1 mL;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	Daporinad Daporinad MedChemExpress (MCE) HY-50876 658084-64-1 FK866 Descriptions Daporinad Daporinad MedChemExpress (MCE) HY-50876 658084-64-1 FK866 APO866 99.72% Powder -20掳C 3 years 4掳C 2 years In solvent -80掳C 2 years -20掳C 1 year Room temperature in continental US may vary elsewhere. Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase Nampt) with an IC50 of 0.09 nM. 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]. 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]. CB17-SCID mice (28-35 days old) are irradiated (200 cGy), and then inoculated subcutaneously in the right flank with 3脳106聽MM1S cells in 100 渭L 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脳width2脳0.5. Tumor growth inhibition (TGI) is calculated. Animals are killed when tumors reach 2 cm3聽or the mice appear moribund. Survival is evaluated from the first day of treatment until death. MM1S cells (2脳104聽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 渭Ci/well) during the last 8 hours of cultures. IC50: 0.09 nM (NMPRTase) Cellular Effect Cell Line Type Value Description 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]
Supplier Website	http://www.medchemexpress.com/FK866.html
Last Update	2025-10-14 16:03:33

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