Nampt-IN-18
Nampt-IN-18 (Compound Q24) is an orally active NAMPT inhibitor with an IC50 of 8.0 nM against hNAMPT. Nampt-IN-18 inhibits NAMPT enzymatic activity. Nampt-IN-18 inhibits DNA synthesis and induces Apoptosis. Nampt-IN-18 exhibits anticancer activity against gastric cancer and colorectal cancer. Nampt-IN-18 can be used for the research of gastrointestinal cancers.
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- Formel: C27H30FN5O2
- Molecular Weight:475.56
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
IC50: 8.0 nM against hNAMPT[1]
Nampt-IN-18 (30 min) potently inhibits the enzymatic activity of recombinant hNAMPT, with an IC50 of 8.0 ± 1.9 nM[1].
Nampt-IN-18 (72 h) potently inhibits the viability of HGC-27 gastric cancer cells, with an IC50 of 0.69 ± 0.14 nM[1].
Nampt-IN-18 (72 h) inhibits the viability of LOVO colon cancer cells with an IC50 of 63 ± 12 nM[1].
Nampt-IN-18 (72 h) inhibits the viability of Caco-2 colorectal adenocarcinoma cells, with an IC50 of 6.5 ± 2.2 nM[1].
Nampt-IN-18 (0.25-1 nM; 24 h) inhibits DNA synthesis in HGC-27 gastric cancer cells in a dose-dependent manner, with a strong inhibitory effect observed at 1 nM[1].
Nampt-IN-18 (1-4 nM; 48 h) induces significant G1-phase and G2/M-phase cell cycle arrest in HGC-27 gastric cancer cells[1].
Nampt-IN-18 (1-4 nM; 48 h) induces apoptosis in HGC-27 gastric cancer cells in a dose-dependent manner[1].
Nampt-IN-18 (0.25-1 nM; 24 h) inhibits the migration of HGC-27 gastric cancer cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human gastric cancer HGC-27 cells
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Concentration:1-4 nM
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Incubation Time:48 h
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Result:Induced measurable apoptosis (~5-11% apoptotic cells) at 1-2 nM.
Induced ~53% apoptotic cells at 4 nM.
| Species | Dose | Route | T1/2 | Tmax | Cmax | MRT0-∞ | CL |
|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.g. | 1.86 h | 0.67 h | 67.43 μg/L | 2.51 h | 68.63 L/h/kg |
Nampt-IN-18 (300 mg/kg; i.g.; single dose) is well tolerated in healthy KM mice, with no acute toxicity or organ damage observed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice[1]
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Dosage:3.75 mg/kg; 7.5 mg/kg; 15 mg/kg
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Administration:i.g.; bid; 12 consecutive days
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Result:Achieved a tumor growth inhibition (TGI) rate of 68.9% at 15 mg/kg dose.
Caused no significant body weight loss across all tested doses (15 mg/kg caused transient early weight loss with subsequent recovery to levels not significantly different from the vehicle group).
Reduced terminal tumor weights significantly at all tested doses compared to the vehicle group.
Detected no histopathological abnormalities in the heart, liver, spleen, lung, or kidney at any tested dose.
Chemical Information
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Molecular Weight 475.56
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Formel C27H30FN5O2
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SMILES
O=C(NC1=CC=C([C@H](C)NC(C2=C(N3CCCCC3)C=CC(F)=C2)=O)C=C1)NCC4=CC=CN=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Nampt-IN-18 Related Classifications
HY-181863 Related Classifications
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