NAMPT/IDO1-IN-1
NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel.
For research use only. We do not sell to patients.
- CAS No.: 2247884-06-4
- Formula: C23H24BrFN8O3
- Molecular Weight:559.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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IDO1 233 nM (IC50) |
NAMPT 57.7 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
5.35 μM
Compound: 10e
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Antiproliferative activity against NAMPT inhibitor-resistant A549 cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay
Antiproliferative activity against NAMPT inhibitor-resistant A549 cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay
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[PMID: 36595482] |
NAMPT/IDO1-IN-1 (compound 10e) (10 μM; 48 h) shows antiproliferative activity against A549/R cells in an NAMPT- and IDO1-dependent manner[1].
NAMPT/IDO1-IN-1 (5 μM, 10 μM, 15 μM; 12 d) inhibits colony formation of A549/R cells and promotes the accumulation of intracellular ROS in a dose-dependent manner[1].
NAMPT/IDO1-IN-1 (10 μM; 24 h) reduces NAD+ in A549/R cells in an NAMPT- and IDO1-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NAMPT/IDO1-IN-1 (25 mg/kg; p.o.; single dose) has good p.o. bioavailability and (5 mg/kg; i.v.; single dose) displays moderate overall exposure[1].
NAMPT/IDO1-IN-1 (50, 100, and 200 mg/kg; p.o.; twice daily for 3 weeks) also shows in vivo anti-tumor effect in an A549/R tumor xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude 6-8 week old mice with A549/R cells[1]
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Dosage:50, 100, and 200 mg/kg
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Administration:Oral gavage; twice daily for 3 weeks
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Result:Showed much better inhibitory activity against A549/R xenografts compared with the single agent.
Showed comparable anti-tumor efficacy with the combination of FK866 and epacadostat at dose of 100 mg/kg, while at 200 mg/kg showed better efficacy than the combination group.
Chemical Information
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CAS No. 2247884-06-4
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Molecular Weight 559.39
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Formula C23H24BrFN8O3
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SMILES
BrC(C=C1N/C(C2=NON=C2NCCCCCCNC(C3=CN4C(C=C3)=NC=C4)=O)=N\O)=C(C=C1)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NAMPT/IDO1-IN-1 Related Classifications
HY-148572 Related Classifications
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