NAMPT PROTAC® A7

Tocris Bioscience | Catalog # 7842

Potent and selective nicotinamide phosphoribosyl transferase (NAMPT) Degrader (PROTAC®)
Tocris Bioscience

Key Product Details

Description

Potent and selective nicotinamide phosphoribosyl transferase (NAMPT) Degrader (PROTAC®)
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Product Description

NAMPT PROTAC A7 is a potent and selective intracellular nicotinamide phosphoribosyl transferase (iNAMPT) Degrader (PROTAC®) (IC50 of 9.5 nM against the enzymatic activity of NAMPT). Comprises a potent NAMPT inhibitor joined by a linker to a ligand for Von Hippel-Lindau (VHL) protein. Proteomic analysis of global protein level changes confirms selectivity. NAMPT PROTAC A7 decreases iNAMPT level and the secretion of extracellular NAMPT (eNAMPT) in CT26 or MC38 cells. In CT26 tumor bearing BALB/c mice, the compound degrades tumoral NAMPT, and boosts antitumor immunity by inhibiting tumor infiltrating myeloid-derived suppressive cells.

Antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF4335 and MAB40441.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Product Specifications for NAMPT PROTAC® A7

Molecular Weight

1185.49

Formula

C58H76N10O11S3

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

(2S,4R)-1-((S)-18-(tert-Butyl)-1,16-dioxo-1-(4-((4-((4-(3-(pyridin-3-ylmethyl)thioureido)phenyl)sulfonyl)piperazin-1-yl)methyl)phenyl)-5,8,11,14-tetraoxa-2,17-diazanonadecan-19-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

CAS Number

2484876-94-8

InChI Key

WJRWRYBOCSUYIN-IWIXZVHYSA-N

SMILES

O=C(C1=CC=C(C=C1)CN2CCN(CC2)S(=O)(C3=CC=C(C=C3)NC(NCC4=CN=CC=C4)=S)=O)NCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(N=CS7)C)C=C6)C)=O)=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 23.71 20

Preparing Stock Solutions for NAMPT PROTAC® A7

The following data is based on the product molecular weight 1185.49.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 4.22 mL 21.09 mL 42.18 mL
1 mM 0.84 mL 4.22 mL 8.44 mL
2 mM 0.42 mL 2.11 mL 4.22 mL
10 mM 0.08 mL 0.42 mL 0.84 mL

Calculators

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Background References

References are publications that support the biological activity of the product.

Product Documents for NAMPT PROTAC® A7

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for NAMPT PROTAC® A7

For research use only

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