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Cat. No.: HY-113837

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Flortanidazole

Flortanidazole is a derivative of 2-Nitroimidazole (HY-N0195). Under hypoxic conditions, Flortanidazole accumulates in hypoxic tissues through the reduction of 2-nitroimidazole and the retention of reactive intermediates by viable hypoxic cells. Flortanidazole binds to intracellular macromolecules under hypoxic conditions, thereby enabling quantification of tumor hypoxia. [¹⁸F]Flortanidazole, formed after labeling Flortanidazole with ¹⁸F, is a hypoxic PET imaging tracer and prognostic imaging biomarker. Flortanidazole can be used in the study of non-small cell lung cancer and colorectal cancer.

For research use only. We do not sell to patients.

CAS No.: 1070878-63-5
Formula: C₉H₁₁FN₆O₃
Molecular Weight:270.22

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Flortanidazole Chemical Structure

CAS No.: 1070878-63-5

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Biological Activity
- Description
- In Vivo
Chemical Information
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Biological Activity

Description

All Radionuclide-Drug Conjugates (RDCs) Isoforms :

In Vivo

[¹⁸F]flortanidazole (18.5 MBq; intravenous injection) imaging in a histological satellite study shows that Metformin (HY-B0627) treatment for 48 h results in a non-significant decrease in tumor hypoxia detected by Pimonidazole (HY-105129A) (3.48% vs. 10.79% in the control group)^[2].

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

Animal Model:

CD-1 athymic nude mice (female, 7-9 weeks of age, A549 xenograft model)^[1]
Dosage:

100 mg/kg (metformin hydrochloride); 18.5 MBq (18F-flortanidazole)
Administration:

i.v. (metformin); i.v. bolus (18F-flortanidazole)
Result:

Reduced mean intratumoral 18F-flortanidazole TBR from 3.21 to 2.87 after metformin administration.
Increased median tumor doubling time to 52 days when metformin was combined with radiotherapy, compared to 34 days for radiotherapy alone and 19 days for controls.
Decreased relative tumor volumes in the metformin + radiotherapy group compared to controls from day 7 (0.68 vs. 1.43) and compared to radiotherapy alone from day 12 (0.77 vs. 1.27).
Demonstrated a hazard ratio of 2.0 for every unit increase in baseline TBR for tumor doubling time.
Showed a relative reduction of 72% in the risk of tumor doubling for tumors with baseline TBR ≤2.5 when metformin was added to radiotherapy.

Animal Model:

CD-1 athymic nude mice (female, A549 xenograft model)^[1]
Dosage:

100 mg/kg (metformin hydrochloride); 18.5 MBq (18F-flortanidazole)
Administration:

i.v. (metformin); i.v. (18F-flortanidazole)
Result:

Showed high accumulation of radioactivity in urine (0.23 %ID) and large intestine (2.36 %ID/g) with low blood-pool activity (0.05 %ID/g) in the metformin-treated group.
Observed no significant differences in the 18F-flortanidazole biodistribution profile between metformin-treated mice and controls.

Animal Model:

CD-1 athymic nude mice (female, 6-7 weeks of age)^[2]
Dosage:

18.5 MBq
Administration:

i.v. bolus; single dose; day 0 and day 1
Result:

Decreased tumor-to-background ratio from 2.53 to 2.28, representing approximately 9% reduction.
Increased hazard of tumor doubling by 8.6% per 10.0% increase in tumor-to-background ratio (hazard ratio, 2.39).

Animal Model:

CD-1 athymic nude mice (female, 6-7 weeks of age)^[2]
Dosage:

18.5 MBq
Administration:

i.v. bolus
Result:

Decreased pimonidazole-detected tumor hypoxia at 48 h post-therapy to 3.48% compared to 10.79% in controls.

Chemical Information

CAS No. 1070878-63-5
Molecular Weight 270.22
Formula C₉H₁₁FN₆O₃
SMILES

OCC(CF)N1N=NC(CN2C=CN=C2[N+]([O-])=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. De Bruycker S, et al. F-Flortanidazole Hypoxia PET Holds Promise as a Prognostic and Predictive Imaging Biomarker in a Lung Cancer Xenograft Model Treated with Metformin and Radiotherapy. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 2019 Jan;60(1):34-40.

[2]. De Bruycker S, et al. Effects of metformin on tumor hypoxia and radiotherapy efficacy: a [F]HX4 PET imaging study in colorectal cancer xenografts. EJNMMI research. 2019 Aug 02;9(1):74.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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