CAS: 1702967-37-0; (((S)-1-Carboxy-5-((S)-3-(Naphthalen-2-yl)-2-((1R,4S)-4-((2-(4,7,10-Tris(Carboxymethyl)-1,4,7,10-Tetraazacyclododecan-1-yl)Acetamido)Methyl)Cyclohexane-1-Carboxamido)Propanamido)Pentyl)Carbamoyl)-L-Glutamic Acid
- 英文名称(((S)-1-Carboxy-5-((S)-3-(Naphthalen-2-yl)-2-((1R,4S)-4-((2-(4,7,10-Tris(Carboxymethyl)-1,4,7,10-Tetraazacyclododecan-1-yl)Acetamido)Methyl)Cyclohexane-1-Carboxamido)Propanamido)Pentyl)Carbamoyl)-L-Glutamic Acid
- IUPAC名称(((S)-1-carboxy-5-((S)-3-(naphthalen-2-yl)-2-((1r,4S)-4-((2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetamido)methyl)cyclohexane-1-carboxamido)propanamido)pentyl)carbamoyl)-L-glutamic acid
- CAS编号1702967-37-0
- MFCD编号:MFCD31715458
- FDA UNII编号:4YM1W0EGQ5
- 分子式:C49H71N9O16分子量:1042.15
- 产品CID: 863980
- 同类组份化合物CAS1702967-37-0 (free base)1703749-62-5 (Lu-177 complex)PSMA617 TFA
- 产品分类Life Science → ADC-linkers → ADC-linker | ADCs → ADC Linker with Payload
物理性质
MSDS等安全信息
合成工艺路线路线简述
专利信息
专利号:US-2024082435-A1
优先权日:2021-02-26
标 题 :Solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates and their use as precursors for therapeutic and/or diagnostic agents
发明人：PINTO ARTUR; BONTEMPS ALEXIS; LEMAIRE LUCAS
权利人:TELIX INT INNOVATIONS PTY LTD
摘要:The disclosure provides methods for the solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates. The disclosure also relates to key intermediates of this process and methods for their preparation such as a method of preparing a compound of formula (V). Also disclosed are use of the conjugates as precursors for therapeutic and/or diagnostic agents, including treating and diagnosing prostate cancer.
专利号:WO-2023148680-A1
优先权日:2022-02-04
标 题 :Methods for large scale synthesis of radionuclide complexes
发明人：BARBATO DONATO; BO MICHELE; ROSSETTO MATTIA; TEDESCO MATTIA; VALERIO FEDERICO
权利人:ADVANCED ACCELERATOR APPLICATIONS
摘要:The present disclosure relates to methods of large scale synthesis of radionuclide complex solutions having a high activity for diagnostic and/or therapeutic purposes, their use in the commercial production of radioactive drug substances, and to respective solutions as well as containers comprising said solutions.
专利号:WO-2025088147-A1
优先权日:2023-10-27
标题 :Theranostic psma-targeting ligands for the diagnosis and treatment of psma-expressing cancers and their solid phase synthesis
发明人：Schäfer Martin; BAUDER-WUEST ULRIKE; ROSCHER MAREIKE; REMDE YVONNE; BENEÅ OVÃ?-SCHÄFER MARTINA; BARINKA CYRIL; KUTILOVÃ? ZSÓFIA; MOTLOVÃ? LUCIA
权利人:DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES OEFFENTLICHEN RECHTS
摘要:The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and radiopharmaceuticals for the treatment of various disease states of PSMA-expressing cancers, especially prostate cancer, and metastases thereof. Further the present invention provides synthetic procedures for the synthesis of such PSMA-targeting ligands.
专利号:US-2024025866-A1
优先权日:2020-11-19
标 题:Synthesis of prostate specific membrane antigen (psma) ligands
专利号:CN-116438165-A
优先权日:2020-11-19
标 题:Synthesis of Prostate Specific Membrane Antigen (PSMA) ligands
专利号:EP-4472678-A1
优先权日:2022-02-04
标题 :Methods for large scale synthesis of radionuclide complexes
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Rathke H, Holland-Letz T, Mier W, Flechsig P, Mavriopoulou E, Röhrich M, Kopka K, Hohenfellner M, Giesel FL, Haberkorn UA, Kratochwil C. Response prediction of (177)Lu-PSMA-617 RLT using PSA, Chromogranin A, and LDH. J Nucl Med. 2019 Oct 25. pii: jnumed.119.231431. doi: 10.2967/jnumed.119.231431. [Epub ahead of print] doi: 10.1186/s13058-019-1205-1.
3: Hofman MS, Emmett L, Violet J, Y Zhang A, Lawrence NJ, Stockler M, Francis RJ, Iravani A, Williams S, Azad A, Martin A, McJannett M; ANZUP TheraP team, Davis ID. TheraP: a randomized phase 2 trial of (177) Lu-PSMA-617 theranostic treatment vs cabazitaxel in progressive metastatic castration-resistant prostate cancer (Clinical Trial Protocol ANZUP 1603). BJU Int. 2019 Oct 22. doi: 10.1111/bju.14876. [Epub ahead of print] pii: E450. doi: 10.3390/pharmaceutics11090450. doi: 10.1186/s13550-019-0548-z.
12: Thang SP, Violet J, Sandhu S, Iravani A, Akhurst T, Kong G, Ravi Kumar A, Murphy DG, Williams SG, Hicks RJ, Hofman MS. Poor Outcomes for Patients with Metastatic Castration-resistant Prostate Cancer with Low Prostate-specific Membrane Antigen (PSMA) Expression Deemed Ineligible for (177)Lu-labelled PSMA Radioligand Therapy. Eur Urol Oncol. 2018 Dec 13. pii: S2588-9311(18)30205-0. doi: 10.1016/j.euo.2018.11.007. [Epub ahead of print] doi: 10.7150/thno.35759. eCollection 2019.
合成参考文献
参考文献:10.1021/acs.jmedchem.4c00332
摘要:Müller M, Lucaroni L, Favalli N, Bassi G, Neri D, Cazzamalli S, Oehler S. Discovery of Glutamate Carboxypeptidase III Ligands to Compete the Uptake of [177Lu]Lu-PSMA-617 in Healthy Organs. J Med Chem. 2024 May 23;67(10):8247–60. doi: 10.1021/acs.jmedchem.4c00332.
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