2. Metabolic Enzyme/Protease
  3. Indoleamine 2,3-Dioxygenase (IDO) NAMPT
  4. 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.

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NAMPT/IDO1-IN-1 Chemical Structure

NAMPT/IDO1-IN-1 Chemical Structure

CAS No. : 2247884-06-4

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NAMPT/IDO1-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

IDO1

233 nM (IC50)

NAMPT

57.7 nM (IC50)

In Vitro

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 Related Antibodies
In Vivo

NAMPT/IDO1-IN-1 (compound 10e) (5 μM; 24 h) shows ROS-boosting effect in Zebrafish embryos, led to a level of ROS much higher than that of LPS (50 μg/mL)[1].
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.

Animal Model: Female nude 6-8 week old mice with A549/R cells[1]
Dosage: 50, 100, and 200 mg/kg
Administration: Oral gavage; twice daily for 3 weeks
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.
Molecular Weight

559.39

Formula

C23H24BrFN8O3
CAS No.
SMILES

BrC(C=C1N/C(C2=NON=C2NCCCCCCNC(C3=CN4C(C=C3)=NC=C4)=O)=N\O)=C(C=C1)F
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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NAMPT/IDO1-IN-1 Related Classifications

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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.

Keywords:

NAMPT/IDO1-IN-12247884-06-4Indoleamine 2,3-Dioxygenase (IDO)NAMPTNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorInhibitorinhibitorinhibit

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