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658084-64-1 1198425-96-5

658084-64-1

658084-64-1 structure
658084-64-1 structure
  • Name: FK866 (APO866, Daporinad)
  • Chemical Name: (E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-pyridin-3-ylprop-2-enamide
  • CAS Number: 658084-64-1
  • Molecular Formula: C24H29N3O2
  • Molecular Weight: 391.506
  • Catalog: Biochemical Inhibitor Metabolism Transferase inhibitor
  • Create Date: 2018-12-05 16:40:03
  • Modify Date: 2024-01-02 20:04:23
  • FK866 is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) with an IC50 of 0.09 nM.
Name (E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-pyridin-3-ylprop-2-enamide
Synonyms 2gvj
Daporinad
2-Propenamide, N-[4-(1-benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-, (2E)-
(2E)-N-[4-(1-Benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)acrylamide
FK866 (APO866, Daporinad)
FK 866
FK866 (APO866,Daporinad)
APO866
(E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE
FK866
Description FK866 is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) with an IC50 of 0.09 nM.
Related Catalog
Target

IC50: 0.09 nM (NMPRTase)
In Vitro Nampt inhibition with FK866 induces significant NAD+ intracellular reduction and selectively kills MM cells. 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 FK866 sensitivity. FK866 abrogates the survival advantage conferred by the bone marrow microenvironment[1]. 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. FK866 reduces the Ca2+ content of TG-responsive Ca2+ stores in Jurkat cells but not in Bcl2-Jurkat cells[2]. Inhibition of NAMPT by FK866, or inhibition of SIRT by nicotinamide decreases proliferation and triggered death of 293T cells involving the p53 acetylation pathway[3].
In Vivo 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].
Cell Assay 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.
Animal Admin 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 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.
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.

[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.

[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.
Density 1.1±0.1 g/cm3
Boiling Point 629.9±51.0 °C at 760 mmHg
Molecular Formula C24H29N3O2
Molecular Weight 391.506
Flash Point 334.8±30.4 °C
Exact Mass 391.225983
PSA 62.30000
LogP 2.45
Appearance white to beige
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.589
Storage condition ?20°C
Water Solubility DMSO: soluble10mg/mL, clear
Hazard Codes Xn
Risk Phrases 22

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title: CAS No. 658084-64-1 | Chemsrc address: https://www.chemsrc.com/en/baike/672603.html

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