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Merck

905224

Sigma-Aldrich

Pomalidomide-PEG6-butyl amine hydrochloride

≥95%

别名:

24-Amino-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin, Crosslinker–E3 Ligase ligand conjugate, Pomalidomide-2-2-2-2-2-2-6-NH2 HCl salt, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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About This Item

经验公式(希尔记法):
C31H46N4O11 · xHCl
分子量:
650.72 (free base basis)
分類程式碼代碼:
12352101
NACRES:
NA.22

ligand

pomalidomide

化驗

≥95%

形狀

powder or crystals

反應適用性

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

官能基

amine

儲存溫度

2-8°C

SMILES 字串

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCCOCCOCCOCCOCCOCCCCCCN)=O)=O)NC1=O.Cl

應用

Partial PROTAC Pomalidomide-PEG6-butyl amine (HCl salt) enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant amine for reactivity with a carboxyl group on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other Partial PROTACs with a pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Protein degrader builiding block Pomalidomide-PEG6-Butyl Amine (HCl salt) enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant amine for reactivity with a carboxyl group on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

法律資訊

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

相關產品

产品编号
说明
价格

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Targeted protein degradation by small molecules.
Bondeson DP and Crews CM
Annual Review of Pharmacology and Toxicology, 57(9), 107-123 (2017)
Targeted protein degradation by PROTACs.
Neklesa TK, et al.
Pharmacology & Therapeutics, 174, 138-144 (2017)
Impact of linker length on the activity of PROTACs.
Cyrus K, et al.
Molecular Biosystems, 7(2), 359-364 (2011)
Targeted protein degradation: from chemical biology to drug discovery.
Cromm, Philipp M and Crews, Craig M
Cell Chemical Biology, 24(9), 1181-1190 (2017)

商品

Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

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