1. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis
  2. NAMPT DNA/RNA Synthesis Apoptosis
  3. 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.

For research use only. We do not sell to patients.

Nampt-IN-18

Nampt-IN-18 Chemical Structure

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Description

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[1].

IC50 & Target

IC50: 8.0 nM against hNAMPT[1]

In Vitro

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.

Apoptosis Analysis[1]

Cell Line: Human gastric cancer HGC-27 cells
Concentration: 1-4 nM
Incubation Time: 48 h
Result: Induced measurable apoptosis (~5-11% apoptotic cells) at 1-2 nM.
Induced ~53% apoptotic cells at 4 nM.
Parmacokinetics
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
In Vivo

Nampt-IN-18 (3.75-15 mg/kg; i.g.; twice daily; for 12 consecutive days) exhibits potent in vivo anti-tumor activity in the HGC-27 gastric cancer xenograft model[1].
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.

Animal Model: BALB/c nude mice[1]
Dosage: 3.75 mg/kg; 7.5 mg/kg; 15 mg/kg
Administration: i.g.; bid; 12 consecutive days
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.
Molecular Weight

475.56

Formula

C27H30FN5O2

SMILES

O=C(NC1=CC=C([C@H](C)NC(C2=C(N3CCCCC3)C=CC(F)=C2)=O)C=C1)NCC4=CC=CN=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Nampt-IN-18
Cat. No.:
HY-181863
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