4-(6-Methyl-1,2,4,5-tetrazin-3-yl)benzoic acid
Based on 1 Customer Validation
4-(6-Methyl-1,2,4,5-tetrazin-3-yl) benzoic acid is an asymmetric tetrazine derivative and a bioorthogonal reaction partner. 4-(6-Methyl-1,2,4,5-tetrazin-3-yl) benzoic acid can be conjugated with Bevacizumab (HY-P9906) via EDC/NHS activation while retaining the VEGF-binding affinity of the antibody, thus constructing a targeting agent for pretargeted immuno-PET/NIRF imaging.
For research use only. We do not sell to patients.
- CAS No.: 1345866-66-1
- Formula: C10H8N4O2
- Molecular Weight:216.20
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Storage:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
Description
In Vivo
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 mice[1]
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Dosage:20 molar excess relative to Bevacizumab
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Administration:i.v.
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Result:Achieved an average tetrazine-to-bevacizumab molar ratio of 7.9:1.
Maintained similar VEGF-binding affinity to HCT116 cells as unmodified bevacizumab.
Reached 64Cu-NOTA-TD tumor uptake of 3.6 %ID/g at 4 h post-probe injection, with a tumor-to-muscle ratio of 19.5.
Showed tumor uptake of 4.6 %ID/g at 4 h post-probe injection via PET/CT imaging, with a tumor-to-muscle ratio of 7.2, both significantly higher than control mice without bevacizumab−tetrazine pretreatment.\nShowed significant fluorescence signal accumulation in tumor regions on FLECT/CT imaging at 4 h post-injection of TD-Cy5.
Demonstrated no significant tumor fluorescence signal in control mice without bevacizumab−tetrazine pretreatment.
Confirmed bioorthogonal ligation between TD-Cy5 and bevacizumab−tetrazine on HCT116 cell surfaces via immunofluorescence staining.
Chemical Information
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CAS No. 1345866-66-1
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Appearance Solid
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Molecular Weight 216.20
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Formula C10H8N4O2
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SMILES
O=C(O)C=1C=CC(=CC1)C2=NN=C(N=N2)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- 4-(6-Methyl-1,2,4,5-tetrazin-3-yl)benzoic acid
- 1345866-66-1
- Drug Derivative
- norbornene derivatives
- inverse electron-demand Diels-Alder ligation
- inverse electron-demand Diels-Alder cycloaddition
- colorectal cancer
- HCT116 colorectal cancer cells
- pretargeted PET imaging
- VEGF
- Reppe anhydride derivatives
- bevacizumab
- pretargeted immuno-PET/NIRF imaging
- Inhibitor
- inhibitor
- inhibit