STF-118804

製品コードS7316 バッチS731601

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H23N3O4S
分子量 461.53 CAS No. 894187-61-2
Solubility (25°C)* 体外 DMSO 61 mg/mL (132.16 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 STF-118804 is a highly specific NAMPT inhibitor.
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 five 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]

プロトコル(参考用のみ)

キナーゼアッセイ 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 Infinite M100 multimode plate reader.
細胞アッセイ 細胞株 Human cell lines (SEM, MV411, Nalm6, 697, Hal01, REH, SUP-B15 and KP-Y-RL) and primary patient leukemic samples
濃度 ~10 μM
反応時間 72 hours
実験の流れ 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 fluorogenic 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.
動物実験 動物モデル Orthotopic xenograft model of ALL transplanted with MV411 cells
投薬量 25 mg/kg twice daily
投与方法 s.c.

カスタマーフィードバック

Data from [Data independently produced by , , Neurochem Res, 2016, 41(9):2367-79.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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