NOTA-cRY9M
NOTA-cRY9M is a reagent targeting FGFR1 with a Kd value of 58 nM, and exhibits subtype selectivity for FGFR2-4. When radiolabeled as [68Ga]Ga-NOTA-cRY9M, it functions as a stabilizer, imaging contrast enhancer, and tumor-targeting agent, and accumulates in FGFR1-positive non-small cell lung cancer xenograft models. NOTA-cRY9M can be used in studies related to non-small cell lung cancer.
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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: C71H108N26O17
- 分子量:1597.78
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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FGFR1 58 nM (Kd) |
68Ga]Ga-NOTA-cRY9M (74 kBq per well; 15-120 min) exhibits time-dependent, FGFR1-specific cellular uptake in Calu-3 and NCI-H520 NSCLC cells, with significantly lower uptake in FGFR1-negative NCI-H2170 cells[1].
[68Ga]Ga-NOTA-cRY9M (74 kBq per well; 10-11-10-2 M unlabeled peptide; 2 h) exhibits high FGFR1-binding affinity in Calu-3 cells, with an IC50 of 62 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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, 4-5 weeks old, 18-21 g)[1]
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Dosage:3.7 MBq
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Administration:i.v.; single dose
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Result:Achieved peak tumor uptake of 3.69 %ID/g at 10 minutes postinjection, with uptake declining gradually to 3.33 %ID/g by 60 minutes.
Reached a maximum tumor-to-muscle ratio of 5.56 at 60 minutes, with tumor-to-liver and tumor-to-lung ratios reaching approximately 2.3 and 3.3, respectively, at 60 minutes.
Exhibited primarily renal excretion with low hepatic retention.\nAchieved peak tumor uptake of 3.11 %ID/g at 10 minutes postinjection.
Reached a maximum tumor-to-muscle ratio of 4.10 at 60 minutes.
Showed tumor uptake of 2.61 %ID/g in ex vivo biodistribution at 60 minutes.\nAchieved a maximum tumor uptake of 1.20 %ID/g, with a consistently low tumor-to-muscle ratio of 1.42 throughout the 60-minute imaging window.
Showed tumor uptake of 0.91 %ID/g in ex vivo biodistribution at 60 minutes.\nShowed a substantial reduction in [68Ga]Ga-NOTA-cRY9M uptake (1.10 %ID/g) in FGFR1-knockdown Calu-3 xenografts compared to control Calu-3 tumors (3.83 %ID/g), with a corresponding tumor-to-muscle ratio of 2.11 vs. 5.89 in controls.
化学情報
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分子量 1597.78
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分子式 C71H108N26O17
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配列
Cyclo(Arg-Trp-Arg-{Lys(NOTA)}-Gln-Thr-Arg-His-Tyr)
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シーケンスの短縮
Cyclo(RWR-{Lys(NOTA)}-QTRHY)
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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)