NAMPT PROTAC® A7
Tocris Bioscience, part of Bio-Techne | Catalog # 7842
Potent and selective nicotinamide phosphoribosyl transferase (NAMPT) Degrader (PROTAC®)
Key Product Details
Description
Potent and selective nicotinamide phosphoribosyl transferase (NAMPT) Degrader (PROTAC®)
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
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Wu NAMPT-targeting PROTAC promotes antitumor immunity via suppressing myeloid-derived suppressor cell expansion. Acta.Pharm.Sin.B 2022 PMID: 35755293
Product Specific Notices for NAMPT PROTAC® A7
For research use only
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