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安全和法规

917931

A1V2PF2-NHEt-C₆-NH₂

Name: A1V2PF2-NHEt-C<SUB>6</SUB>-NH<SUB>2</SUB>
Brand: ALDRICH

别名:

(S)-1-((S)-2-((S)-2-((6-Aminohexyl)amino)propanamido)-2-cyclohexylacetyl)-N-((S)-1-(ethylamino)-3-(4-fluorophenyl)-1-oxopropan-2-yl)pyrrolidine-2-carboxamide, AVP conjugate for IAP-mediated protein degrader development, SNIPER building block

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About This Item

经验公式（希尔记法）:

C₃₃H₅₃FN₆O₄

分子量:

616.81

MDL编号:

MFCD34166214

UNSPSC代码:

41116105

NACRES:

NA.22

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Slide 1 of 10

1 of 10

Sigma-Aldrich

901765

Dde生物素叠氮化物

Sigma-Aldrich

917443

BocA1V2PF2-NHC₆-NH₂

Sigma-Aldrich

916927

BocA1V1PF2-OC₆-NH₂ hydrochloride

Sigma-Aldrich

900891

偶氮生物素-叠氮化物

Sigma-Aldrich

762024

N-[2-[2-[2-(2-叠氮乙氧基)乙氧基]乙氧基]乙基]生物素胺

Sigma-Aldrich

917214

BocA1V2PF1-NHPEG₃-NH₂

Sigma-Aldrich

917435

BocA1V1PF2-OPEG₁-NH₂hydrochloride

Sigma-Aldrich

919411

CCW16-C6-BocNH

Sigma-Aldrich

917710

A1V1PF2-OEt

Sigma-Aldrich

917222

A1V2PF1-NHEt

ligand

A1V2PF2

质量水平

100

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

C[C@H](NCCCCCCN)C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(NCC)=O)CC2=CC=C(C=C2)F)=O)=O)C3CCCCC3)=O

InChI

1S/C33H53FN6O4/c1-3-36-31(42)27(22-24-15-17-26(34)18-16-24)38-32(43)28-14-11-21-40(28)33(44)29(25-12-7-6-8-13-25)39-30(41)23(2)37-20-10-5-4-9-19-35/h15-18,23,25,27-29,37H,3-14,19-22,35H2,1-2H3,(H,36,42)(H,38,43)(H,39,41)/t23-,27-,28-,29-/m0/s1

InChI key

MIQCHNDVWYGFFD-HPEBZSCQSA-N

应用

Protein degrader building block A1V2PF2-NHEt-C₆-NH₂ enables the synthesis of molecules for targeted protein degradation and SNIPER (specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein erasers) technology. Developed in partnership with ComInnex, this conjugate contains an in silico-derived IAP-recruiting ligand, an alkyl-chain crosslinker, and a pendant amine for reactivity with an acid on a target warhead. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and protein degrader, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a terminal amine, including CRBN and VHL targeted, parallel synthesis can be used to more quickly generate SNIPER and PROTAC^® degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand. Learn more about the novel IAP ligands generated through virtual screening of AVP mimetics in our Technology Spotlight.

Building blocks in this series:
916714 A1V2PF2-NHEt
917931 A1V2PF2-NHEt-C₆-N_H2
916684 A1V2PF2-NHEt-C₁₀-NH₂
916935 A1V2PF2-NHEt-PEG₁-NH₂
917192 A1V2PF2-NHEt-PEG₃-NH₂

Technology Spotlight: Degrader Building Blocks with Inhibitor of Apoptosis Protein (IAP) In Silico-Derived Ligands

其他说明

In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)

SNIPERs−Hijacking IAP activity to induce protein degradation

E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones

法律信息

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

储存分类代码

11 - Combustible Solids

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)

Lot/Batch Number

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Nobumichi Ohoka et al.

The Journal of biological chemistry, 292(11), 4556-4570 (2017-02-06)

Many diseases, especially cancers, result from aberrant or overexpression of pathogenic proteins. Specific inhibitors against these proteins have shown remarkable therapeutic effects, but these are limited mainly to enzymes. An alternative approach that may have utility in drug development relies

E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones.

Tasuku Ishida et al.

SLAS discovery : advancing life sciences R & D, 26(4), 484-502 (2020-11-05)

Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are a new modality of chemical tools and potential therapeutics to understand and treat human disease. A required PROTAC component is a ligand binding to an E3 ubiquitin ligase, which is then joined to another ligand binding to a protein to

SNIPERs-Hijacking IAP activity to induce protein degradation.

Mikihiko Naito et al.

Drug discovery today. Technologies, 31, 35-42 (2019-06-16)

The induction of protein degradation by chimeric small molecules represented by proteolysis-targeting chimeras (PROTACs) is an emerging approach for novel drug development. We have developed a series of chimeric molecules termed specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein

商品

Degrader Building Blocks with IAP In Silico-Derived Ligands

Targeted protein degradation reduces disease-relevant proteins in cells using small molecules, hijacking endogenous proteolysis systems.

Accelerating Protein Degrader Discovery with IAP

Plate of 80 ligands against E3 ligase IAP designed by ComInnex; allows creation of bifunctional targeted protein degraders or molecular glues.

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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A1V2PF2-NHEt-C6-NH2

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表单

反应适用性

官能团

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SMILES字符串

InChI

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WGK

闪点(°F)

闪点(°C)

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文件

分析证书(COA)

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A1V2PF2-NHEt-C₆-NH₂