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NAMPT PROTAC® A7

Catalog #: 7842 Datasheet / COA / SDS
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7842/5
NAMPT PROTAC® A7 | CAS No. 2484876-94-8 | Active Degraders
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Description: Potent and selective nicotinamide phosphoribosyl transferase (NAMPT) Degrader (PROTAC®)

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

Purity: ≥98%

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Biological Activity

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.

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

Technical Data

M.Wt:
1185.49
Formula:
C58H76N10O11S3
Solubility:
Soluble to 20 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2484876-94-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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