生物活性
STF-118804 is a highly specific NAMPT inhibitor.
化学数据
| 分子量 | 461.53 |
| 分子式 | C25H23N3O4S |
| CAS号 | 894187-61-2 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 50 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | Human cell lines (SEM, MV411, Nalm6, 697, Hal01, REH, SUP-B15 and KP-Y-RL) and primary patient leukemic samples |
| 方法 | Human cell lines or lineage negative cord blood cells were seeded into 96-well plates (6?05 cells per milliliter). Adding compounds in increasing concentrations, and incubating cells 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. Viability of cell measurement is also by CellTiter-Fluor. The cell-permeable fluorogenic peptide substrate GF-AFC reagent is added at the dilution of 1:2 , 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. Using Prism software to calculate inhibitory concentration (IC50) . 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. Using CalcuSyn version 2.0 software to calculate IC50 . |
| 浓度 | ~10 μM |
| 处理时间 | 72 hours |
| 动物实验 |
|---|
| 动物模型 | Orthotopic xenograft model of ALL transplanted with MV411 cells |
| 配制 | 20% [w/v] [2-hydroxypropyl]-γ-cyclodextrin/5% [v/v] DMSO |
| 剂量 | 25 mg/kg twice daily |
| 给药处理 | s.c. |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1667 mL | 10.8335 mL | 21.6671 mL |
| 5 mM | 0.4333 mL | 2.1667 mL | 4.3334 mL |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1667 mL |
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