STF-118804 is a highly specific NAMPT inhibitor.
| Cell Experiment | |
|---|---|
| Cell lines | Human cell lines (SEM, MV411, Nalm6, 697, Hal01, REH, SUP-B15 and KP-Y-RL) and primary patient leukemic samples |
| Preparation method | 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 . |
| Concentrations | ~10 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Orthotopic xenograft model of ALL transplanted with MV411 cells |
| Formulation | 20% [w/v] [2-hydroxypropyl]-γ-cyclodextrin/5% [v/v] DMSO |
| Dosages | 25 mg/kg twice daily |
| Administration | s.c. |
| Molecular Weight | 461.53 |
| Formula | C25H23N3O4S |
| CAS Number | 894187-61-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] Szu-Chieh Mei, et al. NAD as a genotype-specific drug target
| Related NAMPT Products |
|---|
| NAMPT degrader-3
NAMPT degrader-3 is a NAMPT degrader, depending on VHL- and proteasome manner. |
| Nampt activator-3
NAMPT activator-3, a NAT derivative, is a NAMPT activator with an EC50 of 2.6 μM and a KD of 132 nM. |
| Nampt-IN-8
Nampt-IN-8 (Compound 10d) is an NAMPT inhibitor with an IC50 of 0.183 μM. Nampt-IN-8 is also a relatively good NQO1 substrate. Nampt-IN-8 induces cell apoptosis and ROS. |
| GNE-618
GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity. |
| GPP78
GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects. |
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