STF-118804

SKU: orb1300559

Description

STF-118804 is a potent and selective inhibitor of NAMPT, demonstrating high efficacy against B-cell acute lymphoblastic leukemia (B-ALL) cell lines with IC50 values below 10 nM. It serves as a valuable research tool for investigating cancer metabolism and has shown anti-leukemic activity in both cellular and animal models of B-ALL.

Research Area

Cancer Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 894187-61-2
• MW: 461.5
• Purity: >98%
• Formula: C₂₅H₂₃N₃O₄S
• SMILES: Cc1oc(nc1CS(=O)(=O)c1ccc(C)cc1)-c1ccc(cc1)C(=O)NCc1cccnc1
• Target: Energy production
• Solubility: Soluble in DMSO (47 mg/ml)

Bioactivity

• Target IC50:
  B-ALL cells:<10 nM.
• 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.
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• 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.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

STF118804, STF-118804, STF 118804, Pre-B cell colony enhancing factor, Visfatin, inhibit, Inhibitor, NAMPT, Nicotinamide phosphoribosyl transferase, PBEF, Apoptosis

Compound Identifiers

PubChem CID

20916937