Ac-crown-TATE
Ac-crown-TATE is an actinium-labeled radioligand derived from the SSTR2 agonist crown-TATE, which targets neuroendocrine tumors with high SSTR2 expression. The [226Ac]Ac-crown-TATE form of Ac-crown-TATE possesses both SPECT-detectable γ-emission and α-radiation properties, and it inhibits tumor growth and prolongs survival. Ac-crown-TATE can be used in studies of SSTR2-positive neuroendocrine tumors, targeted α-radiation, and radionuclide imaging.
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- Formel: C69H98N14O21S2
- Molecular Weight:1523.73
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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SSTR2 |
Ac-crown-TATE (125 kBq-4.32 MBq) can be successfully radiolabelled with 226Ac across a range of activity levels to form [226Ac]Ac-crown-TATE[3].
Ac-crown-TATE (1×10-5 M; 30 min) quantitatively radiolabels [225Ac]Ac3+ at room temperature, producing [225Ac]Ac-crown-TATE with a molar activity of 640 kBq/nmol[1].
[225Ac]Ac-crown-TATE (9 days) exhibits high stability in pooled human serum at 37°C, with ≥87% of [225Ac]Ac3+ remaining bound after 9 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ac-crown-TATE ([225Ac]Ac-crown-TATE; 30 or 55 kBq; observation up to 60 days) slows the growth of AR42J tumors and prolongs median survival to 21 and 26 days, respectively, compared with 4 and 5 days in saline and non-radioactive crown-TATE controls[1].
Ac-crown-TATE ([226Ac]Ac-crown-TATE; 58.6 kBq; tail vein injection; 1-48 h) exhibits high tumor uptake in AR42J tumor-bearing NRG mice, reaching 33.1% IA/g at 5 h and remaining at 19.7% IA/g at 48 h, with a tumor absorbed dose coefficient of 222.3 mGy/kBq[2].
Ac-crown-TATE ([226Ac]Ac-crown-TATE; 125, 250 or 375 kBq; observation for up to 60 days) slows tumor growth in AR42J tumor-bearing NRG mice, and extends the median survival time from 7 days (seen in the two control groups) to 16, 24 and 27 days, respectively. No significant body weight loss or toxicity is observed in any dose group[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NRG mice, 3 months old; AR42J xenografts established by s.c. inoculation of 8 × 106 cells in the left shoulder[1]
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Dosage:[225Ac]Ac-crown-TATE 30 kBq, 100 μL; 1, 4, 24, 48, 120 h
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Administration:i.v.; single dose
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Result:Tumor uptake was 7.8% IA/g at 1 h and 11.1% IA/g at 4 h, and remained > 5% IA/g at 120 h.
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Animal Model:Male NRG mice bearing AR42J xenografts[1]
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Dosage:[225Ac]Ac-crown-TATE 30 or 55 kBq; monitored for up to 60 days
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Administration:i.v.; single dose
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Result:Median survival was 21 and 26 days, versus 4 and 5 days for saline and crown-TATE controls.
The 30 kBq dose slowed or stabilized tumor growth; the 55 kBq dose decreased tumor size in 7/9 mice.
Significant weight loss occurred in treatment groups.
Chemical Information
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Molecular Weight 1523.73
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Formel C69H98N14O21S2
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Sequence
Ac-{crown}-{D-Phe}-Cys-Tyr-{D-Trp}-Lys-Thr-Cys-Thr
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Sequence Shortening
Ac-{crown}-{D-Phe}-CY-{D-Trp}-KTCT
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)