•Tirapazamine

Inhibitors

Product Data Sheet

Screening Libraries

CAS No.:27314-97-2

Molecular Formula:

C7H6N4O2

Molecular Weight:

178.15

Target:

DNA/RNA Synthesis

Pathway:

Cell Cycle/DNA Damage

Storage:

PowderIn solvent-20°C

3 years

4°C

2 years-80°C

6 months-20°C

1 monthProteins

HY-13767•

Cat. No.:SOLVENT & SOLUBILITY
In Vitro

DMSO : 62.5 mg/mL (350.83 mM; Need ultrasonic)

Solvent

Mass
1 mg

5 mg

10 mg

1 mM

5.6132 mL

28.0662 mL

56.1325 mL

5 mM

1.1226 mL

5.6132 mL

11.2265 mL10 mM

0.5613 mL

2.8066 mL

5.6132 mL

Concentration
Preparing
Stock Solutions

Please refer to the solubility information to select the appropriate solvent.
In Vivo

1. Add each solvent one by one: 50% PEG300 >> 50% saline
Solubility: 10 mg/mL (56.13 mM); Suspended solution; Need ultrasonic
2. Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: 2.5 mg/mL (14.03 mM); Suspended solution; Need ultrasonic
3. Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline
Solubility: ≥ 2.08 mg/mL (11.68 mM); Clear solution
4. Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (11.68 mM); Clear solution

BIOLOGICAL ACTIVITY
Description

Tirapazamine (SR259075) is an anticancer agent that shows selective cytotoxicity for hypoxic cells in solid tumors, thereby
inducing single-and double-strand breaks in DNA, base damage, and cell death. Tirapazamine is an anticancer andbioreductive agent.Tirapazamine (SR259075) can enhance the cytotoxic effects of ionizing radiation in hypoxic cells[1][2].

In Vitro

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Tirapazamine (SR259075) is the optimal drug for combination therapy using Pba[1].

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MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]

In Vivo

Cell Line:

SCC7 cells

Concentration:

1mg

Incubation Time:

24 hResult:Showed synergism with Pba at ED50, ED90 and ED95.

Tirapazamine (SR259075) (1mg; intravenously injected; twice at a 24-h interval) shows a synergetic effect to kill tumor cells
because TPZ was activated under the hypoxic conditions that originated from the PDT with Pba and laser irradiation[1].
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:

C3H/HeN mice[1].

Dosage:1mg

Administration:

Tirapazamine (1mg; intravenously injected; twice at a 24-h interval)

Result:Suppressed the tumors of mice by using laser irradiation.

CUSTOMER VALIDATION• Biomaterials. 2022 Sep 27;290:121821.
• J Control Release. 2022 Sep 22;351:151-163.
• J Nanobiotechnology. 2024 Jun 21;22(1):358.
• Acta Biomater. 2023 Apr 21;S1742-7061(23)00220-9.
• Front Bioeng Biotechnol. 2022 Feb 21;10:796820.
See more customer validations on www.MedChemExpress.com

REFERENCES[1]. Lee, Donghyun, et al. Optimized Combination of Photodynamic Therapy and Chemotherapy Using Gelatin Nanoparticles Containing Tirapazamine and Pheophorbide
a. ACS applied materials & interfaces vol. 13,9 (2021): 10812-10821.
[2]. Romero, José, et al. Electronic structure and reactivity of tirapazamine as a radiosensitizer. Journal of molecular modeling vol. 27,6 177. 22 May. 2021.
[3]. Cai TY, et al. Tirapazamine sensitizes hepatocellular carcinoma cells to topoisomerase I inhibitors via cooperative modulation of hypoxia-inducible factor-1α. MolCancer Ther. 2014 Mar;13(3):630-42.
[4]. Sliwinska J, et al. Tirapazamine-doxorubicin interaction referring to heart oxidative stress and Ca2? balance protein levels. Oxid Med Cell Longev. 2012;2012:890826.

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Caution: Product has not been fully validated for medical applications. For research use only.
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