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STF-118804

Catalog No. T6682   CAS 894187-61-2
Synonyms: STF118804, STF 118804

STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.

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STF-118804, CAS 894187-61-2
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.
Targets&IC50 B-ALL:<10 nM.
In vitro STF-118804 reduces the viability of B-ALL cell lines containing MLL chromosomal translations, with IC50 values in the low nanomolar range. In addition, leukemic samples from ?ve pediatric ALL patients are also sensitive to STF-118804 in the low nanomolar range. STF-118804 induces leukemia MV411 cell apoptosis without antecedent cell cycle arrest. [1]
In vivo STF-118804 (25 mg/kg twice daily, s.c.) improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia, and effectively depletes leukemia-initiating cells. [1]
Kinase Assay Enzyme Assays: The enzymatic activities of NAMPT and NMNAT are measured using in vitro kits and using the Two-Step Method per manufacturer's instructions. Compounds, NAMPT and/or NMNAT enzymes, and their substrates are mixed and incubated at 30°C for 1 hour. Reagents for the indicator reaction (Wst-1) are then added, and absorbance is read at 450 nm every 5 min at 30°C on a Tecan In?nite M100 multimode plate reader.
Cell Research Human cell lines or lineage negative cord blood cells were seeded into 96-well plates (6×105 cells per milliliter). Compounds are added in increasing concentrations, and cells are incubated at 37°C/5% CO2 for 72 hours. To detect viability, CellTiter-Blue reagent is added at 1:10 dilution, and plates are incubated for 4 hours at 37°C/5% CO2 prior to reading on a Flexstation II 384 or a Synergy H1 reader at an excitation of 555 nm and emission detection of 590 nm. Cell viability is also measured by CellTiter-Fluor. The cell-permeable ?uorogenic peptide substrate GF-AFC reagent is added at 1:2 dilution, and plates are incubated for 30 min at 37°C/5% CO2 prior to reading on a Synergy H1 reader at an excitation of 380 nm and emission detection of 505 nm. Cord blood cells are enumerated on a hemocytometer, and cell viability is assessed with trypan blue exclusion dye. Inhibitory concentration (IC50) is calculated using Prism software. Primary patient samples are plated in 96-well plates and treated with increasing concentrations of STF-118804 for 48 hours at 37°C in 5% CO2. WST-1 reagent is added to the culture medium (1:10 dilution), and absorbance is measured at 450 nm using a Bio-Rad model 680 microplate reader. All assays are performed in triplicate. IC50 is calculated using CalcuSyn version 2.0 software.(Only for Reference)
Synonyms STF118804, STF 118804
Molecular Weight 461.54
Formula C25H23N3O4S
CAS No. 894187-61-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 46.2 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Matheny CJ, et al. Chem Biol. 2013, 20(11), 1352-1363.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Inhibitor Library Anti-Metabolism Disease Compound Library Anti-COVID-19 Compound Library Stem Cell Differentiation Compound Library Apoptosis Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library

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Keywords

STF-118804 894187-61-2 代谢 凋亡 Apoptosis NAMPT Inhibitor STF118804 inhibit Pre-B cell colony enhancing factor Nicotinamide phosphoribosyl transferase PBEF Visfatin STF 118804 inhibitor