| Identification | Back Directory | [Name]
D-Tyrosinamide, 4-chloro-N-[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]-L-phenylalanyl-D-cysteinyl-4-[[[(4S)-hexahydro-2,6-dioxo-4-pyrimidinyl]carbonyl]amino]-L-phenylalanyl-4-[(aminocarbonyl)amino]-D-phenylalanyl-L-lysyl-L-threonyl-L-cysteinyl-, cyclic (2→7)-disulfide | [CAS]
1039726-31-2 | [Synonyms]
DOTA satoreotide/Satoreotide tetraxetan
D-Tyrosinamide, 4-chloro-N-[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]-L-phenylalanyl-D-cysteinyl-4-[[[(4S)-hexahydro-2,6-dioxo-4-pyrimidinyl]carbonyl]amino]-L-phenylalanyl-4-[(aminocarbonyl)amino]-D-phenylalanyl-L-lysyl-L-threonyl-L-cysteinyl-, cyclic (2→7)-disulfide | [Molecular Formula]
C74H98ClN19O21S2 | [MOL File]
1039726-31-2.mol | [Molecular Weight]
1689.28 |
| Chemical Properties | Back Directory | [density ]
1.52±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
1.83±0.10(Predicted) | [color ]
White to off-white | [Sequence]
DOTA-[p-Cl-Phe-cyclo(D-Cys-Phe-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr-NH2] |
| Hazard Information | Back Directory | [Uses]
DOTA-JR11 is a somatostatin receptor 2 （SSTR2）antagonist. DOTA-JR11 can be labeled by 68Ga, used for paired imaging in neuroendocrine tumors (NETs) research[1]. DOTA-JR11 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs). | [in vivo]
[68Ga]Ga-DOTA-JR11 (1.85 MBq, i.v., single dose) shows high tumor uptake in HEK293-SSTR2 tumor model mice, suitable for tumor imaging[2]. | Animal Model: | HEK293-SSTR2 tumor mice model[2] | | Dosage: | 1.85 MBq | | Administration: | Intravenous injection (i.v.), single dose, measured at 5, 30, 60, and 120 min | | Result: | Caused tumor uptake to peak at 60 minutes, significantly higher than uptake in other organs. |
| [IC 50]
RDC Peptide | [References]
[1] Krebs S, et al. Comparison of?68Ga-DOTA-JR11 PET/CT with dosimetric?177Lu-satoreotide tetraxetan (177Lu-DOTA-JR11) SPECT/CT in patients with metastatic neuroendocrine tumors undergoing peptide receptor radionuclide therapy. Eur J Nucl Med Mol Imaging. 2020 Dec;47(13):3047-3057. DOI:10.1007/s00259-020-04832-9
[2] Xie Q, et al. Synthesis, preclinical evaluation, and a pilot clinical imaging study of [18F]AlF-NOTA-JR11 for neuroendocrine neoplasms compared with [68Ga]Ga-DOTA-TATE. Eur J Nucl Med Mol Imaging. 2021 Sep;48(10):3129-3140. DOI:10.1007/s00259-021-05249-8 |
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YantaiBio
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13758194781 |
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