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MedKoo Cat#: 413858 | Name: PSMA-617 free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PSMA-617, also know as vipivotide tetraxetan. It is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer. PSMA617 possesses a small peptide, which was designed to target prostate-specific membrane antigen (PSMA). PSMA617 demonstrates high radiolytic stability for at least 72 h. PSMA617 has high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined). 177 Lu-PSMA-617 offers a potential additional life-prolonging treatment option for men with mCRPC.

Chemical Structure

PSMA-617 free base
PSMA-617 free base
CAS#1702967-37-0 (free base)

Theoretical Analysis

MedKoo Cat#: 413858

Name: PSMA-617 free base

CAS#: 1702967-37-0 (free base)

Chemical Formula: C49H71N9O16

Exact Mass: 1041.5019

Molecular Weight: 1042.15

Elemental Analysis: C, 56.47; H, 6.87; N, 12.10; O, 24.56

Price and Availability

Size Price Availability Quantity
2mg USD 550.00 2 Weeks
5mg USD 1,250.00 2 Weeks
10mg USD 2,250.00 2 Weeks
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Related CAS #
1702967-37-0 (free base) PSMA617 TFA
Synonym
Vipivotide tetraxetan; WHO11010; WHO-11010; WHO 11010; PSMA617; PSMA 617; PSMA-617;
IUPAC/Chemical Name
N-((N6-(3-(Naphthalen-2-yl)-N-(trans-4-((2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetamido)methyl)cyclohexane-1-carbonyl)-L-alanyl)-llysin-N2-yl)carbonyl)-L-glutamic acid
InChi Key
JBHPLHATEXGMQR-LFWIOBPJSA-N
InChi Code
InChI=1S/C49H71N9O16/c59-40(28-55-17-19-56(29-42(62)63)21-23-58(31-44(66)67)24-22-57(20-18-55)30-43(64)65)51-27-32-8-12-35(13-9-32)45(68)52-39(26-33-10-11-34-5-1-2-6-36(34)25-33)46(69)50-16-4-3-7-37(47(70)71)53-49(74)54-38(48(72)73)14-15-41(60)61/h1-2,5-6,10-11,25,32,35,37-39H,3-4,7-9,12-24,26-31H2,(H,50,69)(H,51,59)(H,52,68)(H,60,61)(H,62,63)(H,64,65)(H,66,67)(H,70,71)(H,72,73)(H2,53,54,74)/t32-,35-,37-,38-,39-/m0/s1
SMILES Code
O=C(O)CC[C@@H](C(O)=O)NC(N[C@@H](CCCCNC([C@H](CC1=CC=C2C=CC=CC2=C1)NC([C@H]3CC[C@H](CNC(CN4CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC4)=O)CC3)=O)=O)C(O)=O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 1,042.15 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
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] PubMed PMID: 31653712. 2: Morgenroth A, Tinkir E, Vogg ATJ, Sankaranarayanan RA, Baazaoui F, Mottaghy FM. Targeting of prostate-specific membrane antigen for radio-ligand therapy of triple-negative breast cancer. Breast Cancer Res. 2019 Oct 22;21(1):116. doi: 10.1186/s13058-019-1205-1. PubMed PMID: 31640747; PubMed Central PMCID: PMC6805467. 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] PubMed PMID: 31638341. 4: Seifert R, Kessel K, Boegemann M, Koehler M, Roll W, Stegger L, Weckesser M, Rahbar K. Additional local therapy of liver metastases in mCRPC patients receiving systemic PSMA targeted therapy. J Nucl Med. 2019 Oct 10. pii: jnumed.119.233429. doi: 10.2967/jnumed.119.233429. [Epub ahead of print] PubMed PMID: 31601703. 5: Kratochwil C, Giesel FL, Heussel CP, Kazdal D, Endris V, Nientiedt C, Bruchertseifer F, Kippenberger M, Rathke H, Leichsenring J, Hohenfellner M, Morgenstern A, Haberkorn U, Duensing S, Stenzinger A. Patients resistant against PSMA-targeting alpha-radiation therapy often harbor mutations in DNA-repair associated genes. J Nucl Med. 2019 Oct 10. pii: jnumed.119.234559. doi: 10.2967/jnumed.119.234559. [Epub ahead of print] PubMed PMID: 31601699. 6: Suman S, Parghane RV, Joshi A, Prabhash K, Bakshi G, Talole S, Banerjee S, Basu S. Therapeutic efficacy, Prognostic variables and Clinical Outcome of (177)Lu-PSMA-617 PRLT in Progressive mCRPC following multiple lines of treatment: prognostic implications of high FDG uptake on dual tracer PET-CT vis-à-vis Gleason Score in such cohort. Br J Radiol. 2019 Oct 10:20190380. doi: 10.1259/bjr.20190380. [Epub ahead of print] PubMed PMID: 31600089. 7: Iravani A, Violet J, Azad A, Hofman MS. Lutetium-177 prostate-specific membrane antigen (PSMA) theranostics: practical nuances and intricacies. Prostate Cancer Prostatic Dis. 2019 Oct 8. doi: 10.1038/s41391-019-0174-x. [Epub ahead of print] Review. PubMed PMID: 31595044. 8: Dos Santos JC, Beijer B, Bauder-Wüst U, Schäfer M, Leotta K, Eder M, Benešová M, Kleist C, Giesel F, Kratochwil C, Kopka K, Haberkorn U, Mier W. Development of Novel PSMA Ligands for Imaging and Therapy with Copper Isotopes. J Nucl Med. 2019 Sep 20. pii: jnumed.119.229054. doi: 10.2967/jnumed.119.229054. [Epub ahead of print] PubMed PMID: 31541034. 9: Kurth J, Krause BJ, Schwarzenböck SM, Bergner C, Hakenberg OW, Heuschkel M. First-in-human dosimetry of gastrin-releasing peptide receptor antagonist [(177)Lu]Lu-RM2: a radiopharmaceutical for the treatment of metastatic castration-resistant prostate cancer. Eur J Nucl Med Mol Imaging. 2019 Sep 3. doi: 10.1007/s00259-019-04504-3. [Epub ahead of print] PubMed PMID: 31482426. 10: Müller C, De Prado Leal M, Dominietto MD, Umbricht CA, Safai S, Perrin RL, Egloff M, Bernhardt P, van der Meulen NP, Weber DC, Schibli R, Lomax AJ. Combination of Proton Therapy and Radionuclide Therapy in Mice: Preclinical Pilot Study at the Paul Scherrer Institute. Pharmaceutics. 2019 Sep 2;11(9). pii: E450. doi: 10.3390/pharmaceutics11090450. PubMed PMID: 31480730. 11: Gosewisch A, Ilhan H, Tattenberg S, Mairani A, Parodi K, Brosch J, Kaiser L, Gildehaus FJ, Todica A, Ziegler S, Bartenstein P, Böning G. 3D Monte Carlo bone marrow dosimetry for Lu-177-PSMA therapy with guidance of non-invasive 3D localization of active bone marrow via Tc-99m-anti-granulocyte antibody SPECT/CT. EJNMMI Res. 2019 Aug 14;9(1):76. doi: 10.1186/s13550-019-0548-z. PubMed PMID: 31414241; PubMed Central PMCID: PMC6694348. 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] PubMed PMID: 31412006. 13: Kessel K, Seifert R, Schäfers M, Weckesser M, Schlack K, Boegemann M, Rahbar K. Second line chemotherapy and visceral metastases are associated with poor survival in patients with mCRPC receiving (177)Lu-PSMA-617. Theranostics. 2019 Jul 9;9(17):4841-4848. doi: 10.7150/thno.35759. eCollection 2019. PubMed PMID: 31410185; PubMed Central PMCID: PMC6691377. 14: Banerjee SR, Kumar V, Lisok A, Chen J, Minn I, Brummet M, Boinapally S, Cole M, Ngen E, Wharram B, Brayton C, Hobbs RF, Pomper MG. (177)Lu-labeled low-molecular-weight agents for PSMA-targeted radiopharmaceutical therapy. Eur J Nucl Med Mol Imaging. 2019 Nov;46(12):2545-2557. doi: 10.1007/s00259-019-04434-0. Epub 2019 Aug 10. PubMed PMID: 31399803. 15: Paller CJ, Piana D, Eshleman JR, Riel S, Denmeade SR, Isaacsson Velho P, Rowe SP, Pomper MG, Antonarakis ES, Luo J, Eisenberger MA. A pilot study of prostate-specific membrane antigen (PSMA) dynamics in men undergoing treatment for advanced prostate cancer. Prostate. 2019 Oct;79(14):1597-1603. doi: 10.1002/pros.23883. Epub 2019 Jul 30. PubMed PMID: 31361358. 16: Müller C, Singh A, Umbricht CA, Kulkarni HR, Johnston K, Benešová M, Senftleben S, Müller D, Vermeulen C, Schibli R, Köster U, van der Meulen NP, Baum RP. Preclinical investigations and first-in-human application of (152)Tb-PSMA-617 for PET/CT imaging of prostate cancer. EJNMMI Res. 2019 Jul 25;9(1):68. doi: 10.1186/s13550-019-0538-1. PubMed PMID: 31346796; PubMed Central PMCID: PMC6658632. 17: Ucar B. Synthesis and characterization of natural lanthanum labelled DOTA-Peptides for simulating radioactive Ac-225 labeling. Appl Radiat Isot. 2019 Nov;153:108816. doi: 10.1016/j.apradiso.2019.108816. Epub 2019 Jul 19. PubMed PMID: 31344650. 18: Abouzayed A, Yim CB, Mitran B, Rinne SS, Tolmachev V, Larhed M, Rosenström U, Orlova A. Synthesis and Preclinical Evaluation of Radio-Iodinated GRPR/PSMA Bispecific Heterodimers for the Theranostics Application in Prostate Cancer. Pharmaceutics. 2019 Jul 23;11(7). pii: E358. doi: 10.3390/pharmaceutics11070358. PubMed PMID: 31340483; PubMed Central PMCID: PMC6680768. 19: Subramaniam RM. Section Editor's Notebook: Prostate Cancer Theranosis in Clinical Practice and in Clinical Trials-(68)Ga-Prostate-Specific Member Antigen (PSMA)-11 PET/CT and (177)Lu-PSMA-617 Therapy. AJR Am J Roentgenol. 2019 Aug;213(2):241-242. doi: 10.2214/AJR.19.21391. PubMed PMID: 31328993. 20: Ray Banerjee S, Minn IL, Kumar V, Josefsson A, Lisok A, Brummet M, Chen J, Kiess A, Baidoo K, Brayton C, Mease RC, Brechbiel M, Sgouros G, Hobbs RF, Pomper MG. Preclinical evaluation of (203/212)Pb-labeled low-molecular-weight compounds for targeted radiopharmaceutical therapy of prostate cancer. J Nucl Med. 2019 Jun 28. pii: jnumed.119.229393. doi: 10.2967/jnumed.119.229393. [Epub ahead of print] PubMed PMID: 31253744.

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