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Merck
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Key Documents

911739

Sigma-Aldrich

C5 Lenalidomide-PEG1-NH2 hydrochloride

≥95%

동의어(들):

2-(2-Aminoethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)acetamide hydrochloride, C5 Lenalidomide conjugate, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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About This Item

실험식(Hill 표기법):
C17H20N4O5 · xHCl
Molecular Weight:
360.36 (free base basis)
UNSPSC 코드:
12352101
NACRES:
NA.22

ligand

C5 Lenalidomide

Quality Level

분석

≥95%

형태

powder

반응 적합성

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

작용기

amine

저장 온도

2-8°C

SMILES string

O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(COCCN)=O)=CC=C31.Cl

애플리케이션

Protein degrader builiding block C5 Lenalidomide-PEG1-NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand with alternative exit vector and a PEGylated crosslinker with pendant amine for reactivity with an acid on the target warhead. Because even slight alterations in ligands, warheads, 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 terminal amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Automate your CRBN-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)

법적 정보

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

관련 제품

제품 번호
설명
가격

픽토그램

Health hazard

신호어

Warning

유해 및 위험 성명서

Hazard Classifications

Repr. 2 - STOT RE 2

표적 기관

Blood

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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시험 성적서(COA)

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문서 라이브러리 방문

Philipp M Cromm et al.
Cell chemical biology, 24(9), 1181-1190 (2017-06-27)
Traditional pharmaceutical drug discovery is almost exclusively focused on directly controlling protein activity to cure diseases. Modulators of protein activity, especially inhibitors, are developed and applied at high concentration to achieve maximal effects. Thereby, reduced bioavailability and off-target effects can

문서

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..

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