Product Name :
FK 866 hydrochloride
Description:
FK 866 hydrochloride is an inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 values ranging between 0.09nM and 27.2nM . NAD plays a vital role in numerous biochemical and biologic processes. Targeting NAD synthesis is thought to be a selective manner to kill cancer cells since cancer cells have a higher rate of NAD turnover compared with normal cells. In the vitro MTT assay using a panel of 41 human hematologic cancer cell lines, most cancer cells are sensitive to low concentrations of FK866. Among these cancer cells, AML cells are most sensitive. FK866 is shown selective to human hematologic malignant cells and the normal human HPCs are resistant to FK866 treatment. It is found that FK866 induces cell death in a caspase-independent pathway but in a dose-dependent manner to induce mitochondrial membrane depolarization. Additionally, FK866 induces cell autophagy dependenting on de novo protein synthesis. FK866 also reduces ATP levels in ML-2 cells due to the inhibition of NAD synthesis. The antitumor efficacy of FK866 is also shown in the in vivo models. FK866 significantly prevents tumor growth both in mice xenografted subcutaneously with AML-M4 and Namalwa cells. Furthermore, FK866 clears tumor cells to below detectable levels and results in 80% survival for a long-term .
CAS:
Molecular Weight:
427.97
Formula:
C24H30ClN3O2
Chemical Name:
(2Z)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-(pyridin-3-yl)prop-2-enamide hydrochloride
Smiles :
Cl.O=C(/C=C\C1=CN=CC=C1)NCCCCC1CCN(CC1)C(=O)C1C=CC=CC=1
InChiKey:
MULSIBUGDPOSHV-AFEZEDKISA-N
InChi :
InChI=1S/C24H29N3O2.ClH/c28-23(12-11-21-8-6-15-25-19-21)26-16-5-4-7-20-13-17-27(18-14-20)24(29)22-9-2-1-3-10-22;/h1-3,6,8-12,15,19-20H,4-5,7,13-14,16-18H2,(H,26,28);1H/b12-11-;
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{Droxidopa} web|{Droxidopa} GPCR/G Protein|{Droxidopa} Protocol|{Droxidopa} Data Sheet|{Droxidopa} custom synthesis|{Droxidopa} Epigenetics}
Additional information:
FK 866 hydrochloride is an inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 values ranging between 0.{{Tebipenem} MedChemExpress|{Tebipenem} Antibiotic|{Tebipenem} Biological Activity|{Tebipenem} Purity|{Tebipenem} manufacturer|{Tebipenem} Epigenetic Reader Domain} 09nM and 27.2nM . NAD plays a vital role in numerous biochemical and biologic processes. Targeting NAD synthesis is thought to be a selective manner to kill cancer cells since cancer cells have a higher rate of NAD turnover compared with normal cells. In the vitro MTT assay using a panel of 41 human hematologic cancer cell lines, most cancer cells are sensitive to low concentrations of FK866. Among these cancer cells, AML cells are most sensitive. FK866 is shown selective to human hematologic malignant cells and the normal human HPCs are resistant to FK866 treatment. It is found that FK866 induces cell death in a caspase-independent pathway but in a dose-dependent manner to induce mitochondrial membrane depolarization. Additionally, FK866 induces cell autophagy dependenting on de novo protein synthesis. FK866 also reduces ATP levels in ML-2 cells due to the inhibition of NAD synthesis.PMID:23319057 The antitumor efficacy of FK866 is also shown in the in vivo models. FK866 significantly prevents tumor growth both in mice xenografted subcutaneously with AML-M4 and Namalwa cells. Furthermore, FK866 clears tumor cells to below detectable levels and results in 80% survival for a long-term .|Product information|Molecular Weight: 427.97|Formula: C24H30ClN3O2|Chemical Name: (2Z)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-(pyridin-3-yl)prop-2-enamide hydrochloride|Smiles: Cl.O=C(/C=C\C1=CN=CC=C1)NCCCCC1CCN(CC1)C(=O)C1C=CC=CC=1|InChiKey: MULSIBUGDPOSHV-AFEZEDKISA-N|InChi: InChI=1S/C24H29N3O2.ClH/c28-23(12-11-21-8-6-15-25-19-21)26-16-5-4-7-20-13-17-27(18-14-20)24(29)22-9-2-1-3-10-22;/h1-3,6,8-12,15,19-20H,4-5,7,13-14,16-18H2,(H,26,28);1H/b12-11-;|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|