WazaGaY-1
WazaGaY-1 is an aza-BODIPY derivative, functions as a NIR-I/NIR-II fluorescent contrast agent. WazaGaY-1 undergoes internalization into tumor cells predominantly via clathrin-coated pits. WazaGaY-1 can be used for the research of glioblastoma, ovarian carcinoma and melanoma (Ex/Em = 685/820 nm).
For research use only. We do not sell to patients.
- Formula: C38H36GaI2N5O2
- Molecular Weight:918.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
WazaGaY-1 (0-500 μM) produces concentration-dependent fluorescence in cell-free media, with highest intensity in lipoprotein-enriched plasmas, enabling detection in both NIR-I and NIR-II windows[1].
WazaGaY-1 (10 μM) enables fluorescence imaging up to 4 mm depth in the NIR-I window and up to 6 mm depth in the NIR-II window in a scattering intralipid solution[1].
WazaGaY-1 (0.1-100 μM; 72 h) is non-toxic to HUVEC, U87MG, and HEK293 cells at concentrations up to 50 μM, with only HEK293 showing cytotoxicity at 100 μM; it reduces U87MG spheroid size at 100 μM without significant cytotoxicity[1].
WazaGaY-1 (10 μM, 50 μg/mL; 30 min-24 h) accumulates in the cytoplasm of U87MG and HEK293 cells over time, with greater accumulation in U87MG cells, and penetrates into the core of U87MG spheroids[1].
WazaGaY-1 (10 μM, 10 μg/mL; 0.5-4 h) is predominantly internalized by U87MG cells via clathrin-coated pits, with additional minor active transport pathways, and shows minimal colocalization with lysosomes or mitochondria[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human endothelial HUVEC, glioblastoma U87MG, renal HEK293 cells; U87MG spheroids
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Concentration:0.1 μM; 1 μM; 5 μM; 10 μM; 25 μM; 50 μM; 100 μM
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Incubation Time:72 h
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Result:Maintained cell viability above 85% for all three cell lines at concentrations from 0.1 to 50 μM in 2D cultures.
Induced cytotoxicity in HEK293 cells at 100 μM in 2D cultures.
Maintained cell viability above 85% and necrotic cell percentage below 2.5% at all tested concentrations in U87MG spheroids.
Reduced U87MG spheroid size to 85% of control at 10 μM and 50% of control at 100 μM.
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Mice[1] | 100 μg | i.v. | 4.8 h |
1. In vivo Imaging
a. Take 10 mM WazaGaY-1 (dissolved in DMSO) stock solution and dilute to 1 mM working solution with sterile PBS.
b. Sterilize the working solution through a 0.2 μm filter. Use immediately or in single-use aliquots and store at -20 °C, avoiding freeze-thaw cycles and exposure to sunlight.
c. Administer intravenously 25–100 μg of WazaGaY-1 (i.e., 27-109 μL working solution) 5–72 hours before imaging.
Note: WazaGaY-1 kinetic studies should be performed for each animal model to determine peak signal time.
WazaGaY-1 (25-100 μg; i.v.; single dose) enables clear in vivo and ex vivo detection of subcutaneous U87MG tumors with tumor-to-muscle ratios up to 20 at 72 hours post-intravenous administration, with the 100 μg dose yielding the highest tumor accumulation and tissue contrast ratios[1].
WazaGaY-1 (100 μg; i.v.; single dose) enables detection of subcutaneous IGROV-1 tumors with tumor-to-muscle ratios up to 20 in the NIR-I window and up to 11.7 in the NIR-II window at 72 hours post-intravenous administration of 100 μg[1].
WazaGaY-1 (100 μg; i.v.; single dose) enables specific detection of intraperitoneal IGROV-1 tumors via NIR-I fluorescence imaging with a significant tumor-to-surrounding tissue ratio of ~1.8 at 48 hours post-intravenous administration of 100 μg, supporting its potential for fluorescence-guided surgery[1].
WazaGaY-1 (100 μg; i.v.; single dose) enables detection of subcutaneous A375 tumors with tumor-to-muscle ratios up to 20 in the NIR-I window and up to 11.7 in the NIR-II window at 72 hours post-intravenous administration of 100 μg, with lower tumor accumulation than U87MG and IGROV-1 tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI nude mice (female, 6 weeks old)[1]
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Dosage:25 μg; 50 μg; 100 μg
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Administration:i.v.; single dose
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Result:Detected U87MG tumors via NIR-I fluorescence (800 nm) from 5 to 72 hours post-injection for all doses.
Increased in vivo tumor-to-surrounding tissue ratios between 5 and 24 hours, stabilizing until 72 hours with ratios slightly above 2 at 24 hours.
Achieved ex vivo tumor-to-skin ratios ranging from 3 to 7.6, tumor-to-muscle ratios ranging from 14.4 to 20, and tumor-to-fat ratios ranging from 13 to 28.7 at 72 hours.
Showed significantly higher tumor-to-fat ratios for the 100 μg dose compared to 25 μg (p=0.002) and 50 μg (p=0.014).
Demonstrated significantly higher tumor fluorescence accumulation in the 100 μg dose group compared to the 25 μg and 50 μg groups (p < 0.001).
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Animal Model:NMRI nude mice (female, 6 weeks old)[1]
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Dosage:100 μg
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Administration:i.v.; single dose
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Result:Detected tumors via NIR-I imaging from 5 to 72 hours post-injection, with in vivo tumor-to-surrounding tissue ratios between 2 and 2.5.
Achieved ex vivo tumor-to-muscle ratios of 7-20 and tumor-to-fat ratios of 15-28 in NIR-I window at 72 hours.
Detected tumors via NIR-II imaging with maximum signal at 5 hours and signal persisting to 72 hours; achieved in vivo tumor-to-surrounding tissue ratios of 2.5, and ex vivo tumor-to-muscle ratios of 5-11.7 and tumor-to-fat ratios of 7-13.2 in NIR-II window at 72 hours.
Showed significantly lower tumor fluorescence accumulation than in U87MG tumors (p < 0.001) in both optical windows.\nShowed significantly higher signal in intraperitoneal tumors compared to surrounding tissue (p=0.0036) via NIR-I fluorescence imaging, with a tumor-to-surrounding tissue ratio of ~1.8 at 48 hours.
Showed no statistically significant difference in signal between tumors and surrounding tissue (p=0.1955) via NIR-II fluorescence imaging, with a tumor-to-surrounding tissue ratio of ~1.6 at 48 hours.
Demonstrated significantly higher NIR-I ratio than NIR-II ratio (p=0.0247).
Enabled clear visualization of tumors via NIR-I fluorescence, while tumors were difficult to identify via visual inspection alone.
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Animal Model:NMRI nude mice (female, 6 weeks old)[1]
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Dosage:100 μg
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Administration:i.v.; single dose
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Result:Detected tumors via NIR-I imaging from 5 to 72 hours post-injection, with in vivo tumor-to-surrounding tissue ratios between 2 and 2.5.
Achieved ex vivo tumor-to-muscle ratios of 7-20 and tumor-to-fat ratios of 15-28 in NIR-I window at 72 hours.
Detected tumors via NIR-II imaging with maximum signal at 5 hours and signal persisting to 72 hours; achieved in vivo tumor-to-surrounding tissue ratios of 2, and ex vivo tumor-to-muscle ratios of 5-11.7 and tumor-to-fat ratios of 7-13.2 in NIR-II window at 72 hours.
Showed significantly lower tumor fluorescence accumulation than in U87MG and IGROV-1 tumors (p < 0.001) in both optical windows.
Chemical Information
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Molecular Weight 918.26
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Formula C38H36GaI2N5O2
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SMILES
C[N+](C)(C1=CC=C(C2=CC(C3=C(C=CC=C3)[O-][Ga+3]4([O-]C5=CC=CC=C65)[N-]7C6=C8)=[N]4C2=NC7=C8C9=CC=C(C=C9)[N+](C)(C)C)C=C1)C.[I-].[I-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WazaGaY-1 Related Classifications
HY-D3432 Related Classifications
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