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ChemicalBook--->CAS DataBase List--->1039726-31-2

1039726-31-2

1039726-31-2 Structure

1039726-31-2 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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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