Bioactivity | DOTA-LM3 TFA 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 TFA is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 TFA and 68 Ga-DOTA-LM3 TFA. 68 Ga-DOTA-LM3 TFA shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 TFA can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis[1][2]. | ||||||
Invitro | 177Lu-DOTA-LM3 TFA 是耐受的。177Lu-DOTA-LM3 TFA 主要存在于全身、肾脏、脾脏和转移灶中,导致器官和肿瘤平均吸收剂量较高[2]。 | ||||||
Name | DOTA-LM3 TFA | ||||||
Sequence | DOTA-[p-Cl-Phe-cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr-NH2] | ||||||
Formula | C71H94ClF3N16O21S2 | ||||||
Molar Mass | 1664.18 | ||||||
Appearance | Solid | ||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||
Storage | Sealed storage, away from moisture and light, under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen) |
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Reference | [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. |