DOTA-LM3

DOTA-LM3 is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo (D-Cys-Tyr-D-4-amino-Phe (carbamoyl) -Lys-Thr-Cys) D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 and 68 Ga-DOTA-LM3. 68 Ga-DOTA-LM3 shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis[1][2]. DOTA-LM3 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs) .

Product Specifications

CAS Number

[1192362-32-5]

UNSPSC

12352209

Target

Radionuclide-Drug Conjugates (RDCs) ; Somatostatin Receptor

Type

Peptides

Related Pathways

Antibody-drug Conjugate/ADC Related; GPCR/G Protein; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/dota-lm3.html

Purity

99.37

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : ≥ 100 mg/mL

Smiles

O=C([C@@H](NC([C@@H](CSSC[C@H](NC([C@](NC([C@@H](NC1=O)CCCCN)=O)([H])[C@H](O)C)=O)C(N[C@@H](C(N)=O)CC2=CC=C(C=C2)O)=O)NC([C@@H](NC(CN3CCN(CCN(CCN(CC3)CC(O)=O)CC(O)=O)CC(O)=O)=O)CC4=CC=C(C=C4)Cl)=O)=O)CC5=CC=C(C=C5)O)N[C@@H]1CC6=CC=C(C=C6)NC(N)=O

Molecular Formula

C69H93ClN16O19S2

Molecular Weight

1550.16

References & Citations

[1]Zhu W, et al. A prospective randomized, double-blind study to evaluate the diagnostic efficacy of 68Ga-NODAGA-LM3 and 68Ga-DOTA-LM3 in patients with well-differentiated neuroendocrine tumors: compared with 68Ga-DOTATATE. Eur J Nucl Med Mol Imaging. 2022 Apr;49 (5) :1613-1622. |[2]Baum RP, et al. First-in-Humans Study of the SSTR Antagonist 177Lu-DOTA-LM3 for Peptide Receptor Radionuclide Therapy in Patients with Metastatic Neuroendocrine Neoplasms: Dosimetry, Safety, and Efficacy. J Nucl Med. 2021 Nov;62 (11) :1571-1581.