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A1V1PF2-OEt-C10-NH2 hydrochloride
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别名
A1V1PF2-OEt-C10-NH2 hydrochloride
Ethyl (S)-2-((S)-1-((S)-2-((S)-2-((10-aminodecyl)amino)propanamido)-3,3-dimethylbutanoyl)pyrrolidine-2-carboxamido)-3-(4-fluorophenyl)propanoate
AVP conjugate for IAP-mediated protein degrader development
SNIPER building block
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C35H58FN5O5 · xHCl |
Molecular weight | 647.86 (free base basis) |
Application【应用】 | Protein degrader building block A1V1PF2-OEt-C10-NH2 hydrochloride 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: 917710 A1V1PF2-OEt 917427 A1V1PF2-OEt-C6-NH2 hydrochloride 917672A1V1PF2-OEt-C10-NH2 hydrochloride 917923 A1V1PF2-OEt-PEG1-NH2 hydrochloride 916676 A1V1PF2-OEt-PEG3-NH2 hydrochloride Technology Spotlight: Degrader Building Blocks with Inhibitor of Apoptosis Protein (IAP) In Silico-Derived Ligands |
Other Notes【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 |
Legal Information【法律信息】 | PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license |
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性质
form【形式】 | powder |
Quality Level【质量水平】 | 100 |
storage temp.【储存温度】 | 2-8℃ |
SMILES string | C[C@H](NCCCCCCCCCCN)C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(OCC)=O)CC2=CC=C(C=C2)F)=O)=O)C(C)(C)C)=O.Cl C[C@H](NCCCCCCCCCCN)C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(OCC)=O)CC2=CC=C(C=C2)F)=O)=O)C(C)(C)C)=O.Cl |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |