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Cat. No.: HY-182567

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Nampt-IN-19

Nampt-IN-19 is an orally active and non-substrate nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with a human K_i of 5.6 nM. Nampt-IN-19 blocks NAD⁺ biosynthesis from Nicotinamide (HY-B0150). Nampt-IN-19 acts as an antiproliferative agent in cancer cells. Nampt-IN-19 has preclinical pharmacokinetic properties supporting oral antitumor activity in mouse xenograft models. Nampt-IN-19 can be used for the research of colorectal cancer.

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

CAS No.: 2109805-79-8
Formula: C₂₅H₃₁N₃O₃
Molecular Weight:421.53

Storage:

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

Nampt-IN-19 Chemical Structure

CAS No.: 2109805-79-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	IC₅₀	24 nM Compound: 52	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay	[PMID: 28610984]

In Vitro

Nampt-IN-19 (52) binds to human NAMPT with a K_i of 5.6 nM^[1].
Nampt-IN-19 inhibits PC-3 human prostate cancer cell viability with an IC₅₀ of 24 nM^[1].
Nampt-IN-19 inhibits CYP3A4 with an IC₅₀ of 16 μM and CYP2C9 with an IC₅₀ of 8.4 μM^[1].
Nampt-IN-19 has a scaled unbound intrinsic clearance of <3.4 L/h/kg in rat microsomes^[1].
Nampt-IN-19 has a scaled unbound intrinsic clearance of 18 L/h/kg in mouse microsomes^[1].
Nampt-IN-19 has a scaled unbound intrinsic clearance of 3.5 L/h/kg in human microsomes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	T_1/2	CL_plasma	CL_unbound	F
Rat^[1]	1 mg/kg	i.v.	4.8 h	0.11 L/h/kg	1.7 L/h/kg	/
Rat^[1]	1 mg/kg	p.o.	/	/	/	100 %

In Vivo

Nampt-IN-19 (52) (15 mg/kg/day; p.o.; 3 on, 4 off; for 21 days) has a TGI rate of 90% in a murine xenograft model using the HCT-116 cell line^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 2109805-79-8
Molecular Weight 421.53
Formula C₂₅H₃₁N₃O₃
SMILES

O=C(N1CC2=C(C1)C=CC=C2)NC3=CC=C(C4CCN(CC4)C(CC(C)(C)O)=O)C=C3
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

Handling Instructions (2659 KB)

References

[1]. Curtin ML, et al. SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT). Bioorg Med Chem Lett. 2017;27(15):3317-3325. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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