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A1V2PF2-NHEt-C6-NH2
产品别名
A1V2PF2-NHEt-C6-NH2
(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
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C33H53FN6O4 |
| Molecular weight | 616.81 |
| Application【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-NH2 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 |
| 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 |
产品性质
| form【形式】 | powder |
| Quality Level【质量水平】 | 100 |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | C[C@H](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 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 |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
