| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Nampt-IN-18 (30 min) effectively inhibited the enzyme activity of recombinant hNAMPT, with an IC50 value of 8.0 ± 1.9 nM[1]. Nampt-IN-18 (72 h) effectively inhibited the activity of HGC-27 gastric cancer cells, with an IC50 value of 0.69 ± 0.14 nM[1]. Nampt-IN-18 (72 h) inhibited the activity of LOVO colon cancer cells, with an IC50 value of 63 ± 12 nM[1]. Nampt-IN-18 (72 h) inhibited the activity of Caco-2 colorectal adenocarcinoma cells, with an IC50 value of 6.5 ± 2.2 nM[1]. Nampt-IN-18 (0.25-1 nM; 24 h) inhibited DNA synthesis of HGC-27 gastric cancer cells in a dose-dependent manner, with the strongest inhibitory effect at a concentration of 1 nM[1]. Nampt-IN-18 (1–4 nM; 48 h) significantly induced cell cycle arrest in the G1 and G2/M phases of HGC-27 gastric cancer cells [1]. Nampt-IN-18 (1–4 nM; 48 h) induced apoptosis in HGC-27 gastric cancer cells in a dose-dependent manner [1]. Nampt-IN-18 (0.25–1 nM; 24 h) inhibited the migration of HGC-27 gastric cancer cells in a dose-dependent manner [1].
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|---|---|
| ln Vivo |
Nampt-IN-18 (3.75–15 mg/kg; gavage; twice daily for 12 days) demonstrated potent in vivo antitumor activity in the HGC-27 gastric cancer xenograft model [1]. Nampt-IN-18 (300 mg/kg; gavage; single dose) was well tolerated in healthy KM mice, with no acute toxicity or organ damage observed [1].
|
| Cell Assay |
Apoptosis analysis [1]
Cell Types: Human gastric cancer HGC-27 cells Tested Concentrations: 1-4 nM Incubation Duration: 48 hours Experimental Results: Measurable apoptosis (approximately 5-11%) was induced at a concentration of 1-2 nM. Approximately 53% apoptosis was induced at a concentration of 4 nM. |
| Animal Protocol |
Animal/Disease Models:BALB/c nude mice [1]
Doses: 3.75 mg/kg; 7.5 mg/kg; 15 mg/kg Route of Administration: Gavage; twice daily for 12 days Experimental Results: The tumor growth inhibition rate (TGI) in the 15 mg/kg dose group reached 68.9%. No significant weight loss was observed in any of the tested dose groups (the 15 mg/kg dose group showed a transient early weight loss, which then recovered to a level not significantly different from the control group). All tested dose groups showed a significant reduction in terminal tumor weight compared to the control group. No histopathological abnormalities were detected in the heart, liver, spleen, lungs, or kidneys in any of the tested dose groups. |
| References |
| Molecular Formula |
C27H30FN5O2
|
|---|---|
| Molecular Weight |
475.56
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(NC1=CC=C([C@H](C)NC(C2=C(N3CCCCC3)C=CC(F)=C2)=O)C=C1)NCC4=CC=CN=C4
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1028 mL | 10.5139 mL | 21.0278 mL | |
| 5 mM | 0.4206 mL | 2.1028 mL | 4.2056 mL | |
| 10 mM | 0.2103 mL | 1.0514 mL | 2.1028 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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