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Merck
모든 사진(2)

Key Documents

911658

Sigma-Aldrich

Pomalidomide-C3-NH2 hydrochloride

≥95%

동의어(들):

4-((3-Aminopropyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride, Crosslinker−E3 ligase ligand conjugate, Pomalidomide 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):
C16H18N4O4 · xHCl
Molecular Weight:
330.34 (free base basis)
UNSPSC 코드:
12352101
NACRES:
NA.22

ligand

pomalidomide

분석

≥95%

형태

powder

반응 적합성

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

작용기

amine

저장 온도

2-8°C

SMILES string

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NCCCN)=O)NC1=O.Cl

애플리케이션

Protein degrader building block Pomalidomide-C3-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 and an alkyl-chain crosslinker with pendant amine for reactivity with an acid 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 terminal amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

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

Danger

유해 및 위험 성명서

Hazard Classifications

Repr. 1B

Storage Class Code

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

Yangbing Li et al.
Journal of medicinal chemistry, 62(2), 448-466 (2018-12-12)
Human murine double minute 2 (MDM2) protein is a primary endogenous cellular inhibitor of the tumor suppressor p53 and has been pursued as an attractive cancer therapeutic target. Several potent, nonpeptide, small-molecule inhibitors of MDM2 are currently in clinical development.
Xing Qiu et al.
Organic letters, 21(10), 3838-3841 (2019-05-09)
An organic base-promoted chemoselective alkylation of lenalidomide with different halides was developed, which offers a novel approach to a highly functionalized lenalidomide-based PROTAC library under mild reaction conditions. DIPEA was found to act as an efficient base to trigger facile
Kedra Cyrus et al.
Molecular bioSystems, 7(2), 359-364 (2010-10-06)
Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations
Momar Toure et al.
Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is

문서

Protein Degrader Building Blocks 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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