NP1
NP1 is a NOTA-chelated linear precursor based on the ROR1-targeting peptide. After labeling with [18F]AlF, NP1 yields [18F]AlF-NP1, a PET imaging probe with excellent ROR1 specificity (KD = 141.7 nM), rapid tumor uptake and high target-to-background ratio, which is suitable for non-invasive visualization of various ROR1-overexpressing tumors.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C96H132TN26O32
- 分子量:2165.25
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Radionuclide-Drug Conjugates (RDCs) アイソフォーム固有の製品をすべて表示
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生物活性
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ROR-α 141.7 nM (Kd) |
[18F]AlF-NP1 (3.125-400 nM; 10-60 min) exhibits specific and high uptake in ROR1-positive MC38 cells, with a KD value of 141.7 nM. It also shows evident uptake in B16F10, A549 and HepG2 cells, and the uptake level in MC38 cells is significantly higher than that in B16F10 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
[18F]AlF-NP1 (3.7 MBq; intravenous injection; single administration) exhibits measurable tumor uptake and target-to-nontarget ratios in A549 lung cancer xenograft mice[1].
[18F]AlF-NP1 (3.7 MBq; intravenous injection; single administration) exhibits high specific tumor uptake and desirable target-to-nontarget ratios in MC38 colon cancer xenograft mice, and is cleared via the kidneys[1].
[18F]AlF-NP1 (3.7 MBq; intravenous injection; single administration) exhibits specific, measurable tumor uptake and target-to-nontarget ratios in B16F10 melanoma allograft mice[1].
[18F]AlF-NP1 (7.4 MBq; intravenous injection; single administration) exhibits renal clearance properties in healthy C57BL/6 mice, with extremely low uptake in other normal tissues[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 6-8 weeks old, subcutaneous xenograft via HepG2 cell injection)[1]
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Dosage:3.7 MBq
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Administration:i.v.; single dose
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Result:Reached ~0.6% ID/g tumor uptake at 30 minutes postinjection.
Achieved ~4 tumor-to-muscle ratio at 30 minutes postinjection.
Achieved ~0.1 tumor-to-kidney ratio at 30 minutes postinjection.
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Animal Model:BALB/c nude (male, 6-8 weeks old, subcutaneous xenograft via A549 cell injection)[1]
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Dosage:3.7 MBq
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Administration:i.v.; single dose
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Result:Reached ~0.5% ID/g tumor uptake at 30 minutes postinjection.
Achieved ~5 tumor-to-muscle ratio at 30 minutes postinjection.
Achieved ~0.05 tumor-to-kidney ratio at 30 minutes postinjection.
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Animal Model:C57BL/6 (male, 6-8 weeks old, subcutaneous allograft via MC38 cell injection)[1]
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Dosage:3.7 MBq; 3.7 MBq plus 100 μg/mouse PR7 (blocking studies)
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Administration:i.v.; single dose
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Result:Reached 2.89% ID/g tumor uptake at 30 minutes postinjection.
Reached 1.32% ID/g tumor uptake at 60 minutes postinjection.
Achieved 2.62 tumor-to-muscle ratio at 60 minutes postinjection.
Reached 27.27% ID/g renal uptake at 30 minutes postinjection.
Reached 17.74% ID/g renal uptake at 60 minutes postinjection.
Reduced tumor uptake significantly when blocked with PR7.
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Animal Model:C57BL/6 (male, 6-8 weeks old, subcutaneous allograft via B16F10 cell injection)[1]
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Dosage:3.7 MBq; 3.7 MBq plus 100 μg/mouse PR7 (blocking studies)
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Administration:i.v.; single dose
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Result:Reached ~0.6% ID/g tumor uptake at 30 minutes postinjection.
Achieved ~3 tumor-to-muscle ratio at 30 minutes postinjection.
Achieved ~0.05 tumor-to-kidney ratio at 30 minutes postinjection.
Reduced tumor uptake significantly when blocked with PR7.
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Animal Model:C57BL/6 (male, 6-8 weeks old, normal healthy)[1]
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Dosage:7.4 MBq
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Administration:i.v.; single dose
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Result:Showed high accumulation in kidneys at 30 and 60 minutes postinjection.
Exhibited extremely low radioactivity in all other organs at 30 and 60 minutes postinjection.
化学情報
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分子量 2165.25
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分子式 C96H132TN26O32
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配列
NOTA-Ser-Asp-Ile-Asn-Asp-Arg-Gln-Ile-Pro-Gly-Tyr-Ser-Thr-Tyr-Trp-Gly-Asp-Phe-NH2
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シーケンスの短縮
NOTA-SDINDRQIPGYSTYWGDF-NH2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)