1. Metabolic Enzyme/Protease
    Autophagy
  2. Nampt
    Autophagy

FK866 (Synonyms: Daporinad; APO866)

Cat. No.: HY-50876 Purity: 99.91%
Data Sheet SDS Handling Instructions

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

For research use only. We do not sell to patients.
FK866 Chemical Structure

FK866 Chemical Structure

CAS No. : 658084-64-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $68 In-stock
5 mg $62 In-stock
10 mg $110 In-stock
50 mg $390 In-stock
100 mg $590 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & 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].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume 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
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

MM1S cells (2×104 cells/well) are cultured for 72 and 96 hours in BMSC-coated 96-well plates in the presence or absence of drug. DNA synthesis is measured by (3H)-thymidine uptake, with (3H)-thymidine added (0.5 μCi/well) during the last 8 hours of cultures. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

CB17-SCID mice (28-35 days old) are irradiated (200 cGy), and then inoculated subcutaneously in the right flank with 3×106 MM1S cells in 100 μL RPMI 1640. After detection of tumor (2 weeks after the injection), 7 mice are treated intraperitoneally with either vehicle or FK866 (30 mg/kg body weight) twice a day for 4 days, repeated weekly over 3 weeks. Caliper measurements of the longest perpendicular tumor diameters are performed twice a week to estimate the tumor volume using the following formula: length×width2×0.5. Tumor growth inhibition (TGI) is calculated. Animals are killed when tumors reach 2 cm3 or the mice appear moribund. Survival is evaluated from the first day of treatment until death. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

391.51

Formula

C₂₄H₂₉N₃O₂

CAS No.

658084-64-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.91%

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Product Name:
FK866
Cat. No.:
HY-50876
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