NIR-ASM
NIR-ASM is a near-infrared fluorescent probe that can cross cell membranes and be activated by NQO1. NIR-ASM can distinguish NQO1-expressing cancer cells from normal cells via fluorescence microscopy and flow cytometry. NIR-ASM generates near-infrared fluorescence with a high signal-to-noise ratio in tumor models with NQO1 activity, enabling the detection of endogenous NQO1 activity in vivo. NIR-ASM is applicable to the research of lung cancer and breast cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- CAS 番号: 2646628-35-3
- 分子式: C33H35N3O3
- 分子量:521.65
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
NQO1 |
体外実験
NIR-ASM is an "on-type" fluorescent probe activatable by NQO1, suitable for cell-free biochemical assays. Its fluorescence response to NQO1 concentration shows a linear relationship within the range of 0.125 to 2.5 μg/mL, with a limit of detection of 0.191 μg/mL and a Km value of 33.82 μM for NQO1[1].
NIR-ASM selectively detects endogenous NQO1 activity in NQO1-positive A549 and NCI-H460 cancer cells, but fails to detect such activity in NQO1-negative IMR-90, HUVEC or untransfected MDA-MB-231 cells, and its activation strictly depends on the expression of NQO1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
NIR-ASM (5 mg/kg; intravenous injection; single administration) selectively generates a near-infrared fluorescent signal in NQO1-positive orthotopic LLC lung tumors of C57BL/6 mice, with the signal peaking at 30 minutes post intravenous administration, while no signal is detected in the lungs of healthy mice[1].
NIR-ASM (5 mg/kg; 5 times per week; for 5 consecutive weeks) does not induce obvious toxicity or histological changes in healthy CD1 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:athymic nude (nu/nu) (female, 4-6 weeks old, subcutaneous xenograft model)[1]
-
Dosage:5 mg/kg
-
Administration:i.v.; single dose
-
Result:Reached a plateau in near-infrared fluorescence signal in the A549 tumor region at 30 minutes post-administration.
Detected no fluorescence signal in other major organs.
Confirmed fluorescence signal was restricted to the tumor via ex vivo imaging.
Detected NQO1 protein only in tumor lysates, not in other tissue lysates via Western blot analysis.
-
Animal Model:C57BL/6 (female, orthotopic metastatic lung cancer model)[1]
-
Dosage:5 mg/kg
-
Administration:i.v.; single dose
-
Result:Reached a maximum near-infrared fluorescence signal in the tumor-bearing lung region at 30 minutes post-administration.
Showed fluorescence signal intensity in tumor-bearing lungs more than 100-fold higher than in other major organs.
Confirmed strong fluorescence signal in tumor-bearing lungs with minimal signal in other organs via ex vivo imaging.
Detected no fluorescence signal in the lungs of non-tumor-bearing mice treated with NIR-ASM.
化学情報
-
CAS 番号 2646628-35-3
-
分子量 521.65
-
分子式 C33H35N3O3
-
SMILES
CC1=C(C(C(C(C)(CC(NC2=CC=C(C=C2)/C=C/C3=C/C(CC(C)(C3)C)=C(C#N)/C#N)=O)C)=C(C1=O)C)=O)C
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
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)