4-(6-Methyl-1,2,4,5-tetrazin-3-yl)benzoic acid

Cat. No.: HY-W422109: Fiche technique
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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.

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4-(6-Methyl-1,2,4,5-tetrazin-3-yl)benzoic acid Chemical Structure

CAS No. : 1345866-66-1

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50 mg	En stock	Estimated Time of Arrival: December 31
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Description

In Vivo

Conjugation of 4-(6-Methyl-1,2,4,5-tetrazin-3-yl) benzoic acid (intravenous injection) with Bevacizumab yields a bevacizumab-tetrazine conjugate. This conjugate retains VEGF-binding affinity, accumulates selectively in HCT116 colorectal tumors, and supports pretargeted PET imaging using ⁶⁴Cu-NOTA-TD to achieve high tumor-to-background contrast, with a tumor-to-muscle ratio reaching 19.5 at 4 h post-probe injection^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c nude mice^[1]
Dosage:	20 molar excess relative to Bevacizumab
Administration:	i.v.
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.

Masse moléculaire

216.20

Formule

C₁₀H₈N₄O₂

CAS No.

1345866-66-1

Appearance

Solid

SMILES

O=C(O)C=1C=CC(=CC1)C2=NN=C(N=N2)C

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Store at room temperature 3 years

In solvent	-80°C	2 years
	-20°C	1 year

Pureté et documentation

Fiche technique (271 KB) SDS (252 KB) Instruction de manipulation (2659 KB)

Références

[1]. Xudong Shi, et al. 64Cu-Based Pretargeted Immuno-Positron Emission Tomography
and Near-Infrared Fluorescence Imaging of the Vascular Endothelial
Growth Factor. ACS Omega 2019, 4, 5310-5316.

[2]. Steffen A. Busche, et al. Tetrazine-norbornene versus azide-norbornene ligation: evaluating the toolbox for polymer-polymer coupling. Polym. Chem., 2023, 14,
2888.