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首页-抗体药物偶连体和PROTACs-PROTAC-NAMPT PROTAC 632005
NAMPT PROTAC 632005

Chemical Structure : NAMPT PROTAC 632005

CAS No.: 3023810-20-7

NAMPT PROTAC 632005

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 897.14
分子式 C51H64N10O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

参考文献

1. Zhu X, et al. Cell Chem Biol. 2024 Jun 20;31(6):1203-1218.e17.

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