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安全和法规

911666

Pomalidomide-C₆-NH₂ hydrochloride

Name: Pomalidomide-C<SUB>6</SUB>-NH<SUB>2</SUB> hydrochloride
Brand: ALDRICH

≥95%

别名:

4-((6-Aminohexyl)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

经验公式（希尔记法）:

C₁₉H₂₄N₄O₄ · xHCl

CAS号:

2375194-37-7

分子量:

372.42 (free base basis)

MDL编号:

MFCD31729298

UNSPSC代码:

12352101

NACRES:

NA.22

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Sigma-Aldrich

901496

Pomalidomide-C₆-CO₂H

Sigma-Aldrich

901513

Pomalidomide-PEG₂-NH₂ hydrochloride

Sigma-Aldrich

901490

(S,R,S)-AHPC hydrochloride

Sigma-Aldrich

901495

Pomalidomide-PEG₃-NH₂ hydrochloride

Sigma-Aldrich

905623

Gold nanospheres

Sigma-Aldrich

P0018

泊马度胺

Sigma-Aldrich

904651

(S,R,S)-AHPC-PEG₃-azide

Sigma-Aldrich

901832

Pomalidomide-PEG₆-NH₂ hydrochloride

Sigma-Aldrich

930520

Pomalidomide-PEG₂-C₂-NH₂ hydrochloride

Sigma-Aldrich

903825

Pomalidomide-PEG1-azide

ligand

pomalidomide

方案

≥95%

表单

powder

反应适用性

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

官能团

amine

储存温度

2-8°C

SMILES字符串

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NCCCCCCN)=O)NC1=O.Cl

InChI

1S/C19H24N4O4.ClH/c20-10-3-1-2-4-11-21-13-7-5-6-12-16(13)19(27)23(18(12)26)14-8-9-15(24)22-17(14)25;/h5-7,14,21H,1-4,8-11,20H2,(H,22,24,25);1H

InChI key

PBGMRXNTLPSDNR-UHFFFAOYSA-N

应用

Protein degrader building block Pomalidomide-C₆-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.

其他说明

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC^® Degraders for Targeted Protein Degradation

Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands

Chemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation Reaction

Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation

Discovery of MD-224 as a First-in-Class, Highly Potent and Efficacious PROTAC MDM2 Degrader Capable of Achieving Complete and Durable Tumor Regression

法律信息

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

警示用语：

Danger

危险声明

H360D

预防措施声明

P201 - P308 + P313

危险分类

Repr. 1B

储存分类代码

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

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

新产品

历史批次信息供参考:

分析证书(COA)

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Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands.

Ziqian Wang et al.

Journal of medicinal chemistry, 62(17), 8152-8163 (2019-08-08)

Proteolysis targeting chimera (PROTAC) recruits an E3 ligase to a target protein to induce its ubiquitination and subsequent degradation. We reported success in the development of two PROTACs (C3 and C5) that potently and selectively induce the degradation of Mcl-1

Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation.

Lijie Peng et al.

ACS medicinal chemistry letters, 10(5), 767-772 (2019-05-18)

A series of (E)-3-(4-((2,4-bis(trifluoromethyl)benzyl)oxy)-3-methoxyphenyl)-2-cyanoacrylamide derivatives were designed and synthesized as new estrogen-related receptor α (ERRα) degraders based on the proteolysis targeting chimera (PROTAC) concept. One of the representative compounds 6c is capable of specifically degrading ERRα protein by >80% at

Chemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation Reaction.

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

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression.

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.

商品

Degrader Building Blocks for Targeted Protein Degradation

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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Pomalidomide-C6-NH2 hydrochloride

≥95%

About This Item

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方案

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反应适用性

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储存温度

SMILES字符串

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储存分类代码

WGK

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分析证书(COA)

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Pomalidomide-C₆-NH₂ hydrochloride