Chemical Structure : NAMPT PROTAC 632005
CAS No.:
3023810-20-7
NAMPT PROTAC 632005
Catalog No.: PC-22769Not For Human Use, Lab Use Only.
NAMPT PROTAC 632005 is a potent, selective, next-generation PROTAC degrader of nicotinamide phosphoribosyltransferase (NAMPT) with DC50 of < 1 nM and Dmax of 98.2% in Jurkat cells, simultaneously degrades iNAMPT and eNAMPT.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
NAMPT PROTAC 632005 is a potent, selective, next-generation PROTAC degrader of nicotinamide phosphoribosyltransferase (NAMPT) with DC50 of < 1 nM and Dmax of 98.2% in Jurkat cells, simultaneously degrades iNAMPT and eNAMPT.
632005 exhibits cell anti-proliferative activity IC50 of 4.6 nM in Jurkat cells.
632005 specifically degrades NAMPT protein in a cereblon- and proteasome-dependent manner.
632005 significantly reduced the protein levels of iNAMPT and concurrently diminished eNAMPT levels.
The toxicity of NAMPT-targeting PROTAC 632005 is mitigated with NA supplementation.
Treatment with the PROTAC 632005 and NA is efficacious against NAPRT-deficient pan-cancers.
Physicochemical Properties
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M.Wt
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897.14
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Formula
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C51H64N10O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(E)-N-(4-(1-(6-(4-(4-(7-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)hept-6-yn-1-yl)piperazin-1-yl)piperidin-1-yl)pyridazine-3-carbonyl)piperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide
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References
1. Zhu X, et al. Cell Chem Biol. 2024 Jun 20;31(6):1203-1218.e17.
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