Cat. No.: HY-13767

Tirapazamine

(Synonyms: SR259075; SR4233; Win59075; SML 0552; SR 259075; Tirazone)

15 Cited Publications

Customer Review

Based on 15 publication(s) in Google Scholar

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 and bioreductive agent.Tirapazamine (SR259075) can enhance the cytotoxic effects of ionizing radiation in hypoxic cells.

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

Purity: 99.02%
CAS No.: 27314-97-2
Formula: C₇H₆N₄O₂
Molecular Weight:178.15

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tirapazamine Chemical Structure

CAS No.: 27314-97-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (15)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

All DNA/RNA Synthesis Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	6.8 μM Compound: Tirapazamine	Cytotoxicity against human A549 cells incubated for 4 hrs in anoxic condition followed by oxic exposure for 48 hrs by sulforhodamine B assay Cytotoxicity against human A549 cells incubated for 4 hrs in anoxic condition followed by oxic exposure for 48 hrs by sulforhodamine B assay	[PMID: 32196334]
A549	GI₅₀	63 μM Compound: Tirapazamine	Cytotoxicity against human A549 cells incubated for 52 hrs in oxic condition by sulforhodamine B assay Cytotoxicity against human A549 cells incubated for 52 hrs in oxic condition by sulforhodamine B assay	[PMID: 32196334]
A549	IC₅₀	>50 μM Compound: TPZ	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation under normoxia conditions after 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation under normoxia conditions after 72 hrs by SRB assay	[PMID: 25468044]
A549	IC₅₀	1.93 μM Compound: TPZ	Cytotoxicity against human A549 cells for 72 hrs under hypoxic condition by MTT assay Cytotoxicity against human A549 cells for 72 hrs under hypoxic condition by MTT assay	[PMID: 21281992]
A549	IC₅₀	6.9 μM Compound: TPZ	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation under hypoxia conditions after 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation under hypoxia conditions after 72 hrs by SRB assay	[PMID: 25468044]
A549	IC₅₀	7.43 μM Compound: TPZ	Cytotoxicity against human A549 cells for 72 hrs under normoxic condition by MTT assay Cytotoxicity against human A549 cells for 72 hrs under normoxic condition by MTT assay	[PMID: 21281992]
COLO 205	IC₅₀	47.7 μM Compound: Tirapazamine	Cytotoxicity against human COLO205 cells measured after 48 hrs under hypoxic condition by CCK8 assay Cytotoxicity against human COLO205 cells measured after 48 hrs under hypoxic condition by CCK8 assay	[PMID: 27140429]
H9c2	EC₅₀	>100 μM Compound: 10; TPZ	Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability incubated for 24 hrs under 19% O2 condition by Hoechst 33342 staining based microscopic analysis Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability incubated for 24 hrs under 19% O2 condition by Hoechst 33342 staining based microscopic analysis	[PMID: 34124675]
HCT-116	IC₅₀	11.9 μM Compound: Tirapazamine	Cytotoxicity against human HCT116 cells measured after 48 hrs under hypoxic condition by CCK8 assay Cytotoxicity against human HCT116 cells measured after 48 hrs under hypoxic condition by CCK8 assay	[PMID: 27140429]
HCT-116	IC₅₀	72.7 μM Compound: Tirapazamine	Cytotoxicity against human HCT116 cells measured after 18 hrs under hypoxic condition by CCK8 assay Cytotoxicity against human HCT116 cells measured after 18 hrs under hypoxic condition by CCK8 assay	[PMID: 27140429]
HepG2	IC₅₀	19.1 μM Compound: TPZ	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 16777409]
HepG2	IC₅₀	56.6 μg/mL Compound: TPZ	Growth inhibition of human HepG2 cells after 48 hrs by SRB assay Growth inhibition of human HepG2 cells after 48 hrs by SRB assay	[PMID: 20236735]
HL-60	IC₅₀	16.1 μM Compound: TPZ	Cytotoxicity against human HL60 cells in normoxia after 48 hrs Cytotoxicity against human HL60 cells in normoxia after 48 hrs	[PMID: 16777409]
HL-60	IC₅₀	2.31 μM Compound: TPZ	Ratio of cytotoxicity against human HL60 cells in normoxia to hypoxia after 48 hrs Ratio of cytotoxicity against human HL60 cells in normoxia to hypoxia after 48 hrs	[PMID: 16777409]
HL-60	IC₅₀	7 μM Compound: TPZ	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 16777409]
HL-60	IC₅₀	7 μM Compound: TPZ	Cytotoxicity against human HL60 cells in hypoxia after 48 hrs Cytotoxicity against human HL60 cells in hypoxia after 48 hrs	[PMID: 16777409]
HT-29	IC₅₀	>50 μM Compound: TPZ	Cytotoxicity against human HT-29 cells after 72 hrs under normoxia conditions by SRB assay Cytotoxicity against human HT-29 cells after 72 hrs under normoxia conditions by SRB assay	[PMID: 25462282]
HT-29	IC₅₀	>50 μM Compound: TPZ	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation under normoxia conditions after 72 hrs by SRB assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation under normoxia conditions after 72 hrs by SRB assay	[PMID: 25468044]
HT-29	IC₅₀	196 μM Compound: 1	Inhibitory concentration against human adenocarcinoma HT-29 cell line under aerobic condition Inhibitory concentration against human adenocarcinoma HT-29 cell line under aerobic condition	[PMID: 12502371]
HT-29	IC₅₀	387 μM Compound: TPZ	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth under normoxia condition by SRB assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth under normoxia condition by SRB assay	[PMID: 28851503]
HT-29	IC₅₀	387 μM Compound: 1	Concentration required to kill aerobic HT-29 human colon carcinoma cells in vitro Concentration required to kill aerobic HT-29 human colon carcinoma cells in vitro	[PMID: 14711317]
HT-29	IC₅₀	5.1 μM Compound: 1, TPZ	Cytotoxicity against human HT29 cells under hypoxic conditions after 4 hrs Cytotoxicity against human HT29 cells under hypoxic conditions after 4 hrs	[PMID: 18001018]
HT-29	IC₅₀	5.1 μM Compound: 1, TPZ	Cytotoxicity against human HT-29 cells after 4 hrs under strict hypoxic condition Cytotoxicity against human HT-29 cells after 4 hrs under strict hypoxic condition	[PMID: 18847185]
HT-29	IC₅₀	5.3 μM Compound: 1	Inhibitory concentration against human adenocarcinoma HT-29 cell line under hypoxic condition Inhibitory concentration against human adenocarcinoma HT-29 cell line under hypoxic condition	[PMID: 12502371]
HT-29	IC₅₀	6.2 μM Compound: TPZ	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth under hypoxia condition by SRB assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth under hypoxia condition by SRB assay	[PMID: 28851503]
HT-29	IC₅₀	6.2 μM Compound: 1	Concentration required to kill hypoxic HT-29 human colon carcinoma cells in vitro Concentration required to kill hypoxic HT-29 human colon carcinoma cells in vitro	[PMID: 14711317]
HT-29	IC₅₀	9.45 μM Compound: TPZ	Cytotoxicity against human HT-29 cells after 72 hrs under hypoxia conditions by SRB assay Cytotoxicity against human HT-29 cells after 72 hrs under hypoxia conditions by SRB assay	[PMID: 25462282]
HT-29	IC₅₀	9.45 μM Compound: TPZ	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation under hypoxia conditions after 72 hrs by SRB assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation under hypoxia conditions after 72 hrs by SRB assay	[PMID: 25468044]
K562	IC₅₀	1.81 μM Compound: TPZ	Cytotoxicity against human K562 cells for 72 hrs under hypoxic condition by MTT assay Cytotoxicity against human K562 cells for 72 hrs under hypoxic condition by MTT assay	[PMID: 21281992]
K562	IC₅₀	19.41 μM Compound: TPZ	Cytotoxicity against human K562 cells for 72 hrs under normoxic condition by MTT assay Cytotoxicity against human K562 cells for 72 hrs under normoxic condition by MTT assay	[PMID: 21281992]
K562	IC₅₀	5.2 μM Compound: TPZ	Cytotoxicity against human K562 cells after 48 hrs by MTT assay Cytotoxicity against human K562 cells after 48 hrs by MTT assay	[PMID: 16777409]
KB	IC₅₀	18.71 μM Compound: TPZ	Cytotoxicity against human KB cells for 72 hrs under hypoxic condition by MTT assay Cytotoxicity against human KB cells for 72 hrs under hypoxic condition by MTT assay	[PMID: 21281992]
KB	IC₅₀	6.29 μM Compound: TPZ	Cytotoxicity against human KB cells for 72 hrs under normoxic condition by MTT assay Cytotoxicity against human KB cells for 72 hrs under normoxic condition by MTT assay	[PMID: 21281992]
MDA-MB-468	IC₅₀	1.304 μM Compound: Tirapazamine	Cytotoxicity against human MDA-MB-468 cells incubated for 4 hrs under hypoxic condition followed by compound washout and measured after 5 days by SRB assay Cytotoxicity against human MDA-MB-468 cells incubated for 4 hrs under hypoxic condition followed by compound washout and measured after 5 days by SRB assay	[PMID: 30885680]
MDA-MB-468	IC₅₀	105.2 μM Compound: Tirapazamine	Cytotoxicity against human MDA-MB-468 cells incubated for 4 hrs under aerobic condition followed by compound washout and measured after 5 days by SRB assay Cytotoxicity against human MDA-MB-468 cells incubated for 4 hrs under aerobic condition followed by compound washout and measured after 5 days by SRB assay	[PMID: 30885680]
MDCK	IC₅₀	<50 μM Compound: Tirapazamine	Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 2 hrs under hypoxic condition by Alamar blue assay Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 2 hrs under hypoxic condition by Alamar blue assay	[PMID: 27823879]
MDCK	IC₅₀	>300 μM Compound: Tirapazamine	Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability preincubated for 2 hrs followed by 72 hrs incubation under normoxic condition by Alamar blue assay Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability preincubated for 2 hrs followed by 72 hrs incubation under normoxic condition by Alamar blue assay	[PMID: 27823879]
MDCK	IC₅₀	>300 μM Compound: Tirapazamine	Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability preincubated for 2 hrs followed by 72 hrs incubation under normoxic condition by Alamar blue assay Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability preincubated for 2 hrs followed by 72 hrs incubation under normoxic condition by Alamar blue assay	[PMID: 27823879]
MDCK	IC₅₀	95 μM Compound: Tirapazamine	Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 2 hrs under hypoxic condition by Alamar blue assay Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 2 hrs under hypoxic condition by Alamar blue assay	[PMID: 27823879]
MOLM-13	EC₅₀	22 μM Compound: 10; TPZ	Cytotoxicity against human MOLM13 cells assessed as reduction in cell viability incubated for 24 hrs under 2% O2 condition by Hoechst 33342 staining based microscopic analysis Cytotoxicity against human MOLM13 cells assessed as reduction in cell viability incubated for 24 hrs under 2% O2 condition by Hoechst 33342 staining based microscopic analysis	[PMID: 34124675]
MOLM-13	EC₅₀	22 μM Compound: 4; TPZ	Antiproliferative activity against human MOLM13 cells after 24 hrs under 2% O2 condition by Hoechst 33342 staining-based UV-microscopic analysis Antiproliferative activity against human MOLM13 cells after 24 hrs under 2% O2 condition by Hoechst 33342 staining-based UV-microscopic analysis	[PMID: 28284865]
MOLM-13	EC₅₀	95 μM Compound: 10; TPZ	Cytotoxicity against human MOLM13 cells assessed as reduction in cell viability incubated for 24 hrs under 19% O2 condition by Hoechst 33342 staining based microscopic analysis Cytotoxicity against human MOLM13 cells assessed as reduction in cell viability incubated for 24 hrs under 19% O2 condition by Hoechst 33342 staining based microscopic analysis	[PMID: 34124675]
MOLM-13	EC₅₀	95 μM Compound: 4; TPZ	Antiproliferative activity against human MOLM13 cells after 24 hrs under 19% O2 condition by Hoechst 33342 staining-based UV-microscopic analysis Antiproliferative activity against human MOLM13 cells after 24 hrs under 19% O2 condition by Hoechst 33342 staining-based UV-microscopic analysis	[PMID: 28284865]
MOLT-4	IC₅₀	15.8 μM Compound: TPZ	Cytotoxicity against human Molt4 cells in normoxia after 48 hrs Cytotoxicity against human Molt4 cells in normoxia after 48 hrs	[PMID: 16777409]
MOLT-4	IC₅₀	3.43 μM Compound: TPZ	Ratio of cytotoxicity against human Molt4 cells in normoxia to hypoxia after 48 hrs Ratio of cytotoxicity against human Molt4 cells in normoxia to hypoxia after 48 hrs	[PMID: 16777409]
MOLT-4	IC₅₀	4.6 μM Compound: TPZ	Cytotoxicity against human Molt4 cells after 48 hrs by MTT assay Cytotoxicity against human Molt4 cells after 48 hrs by MTT assay	[PMID: 16777409]
MOLT-4	IC₅₀	4.6 μM Compound: TPZ	Cytotoxicity against human Molt4 cells in hypoxia after 48 hrs Cytotoxicity against human Molt4 cells in hypoxia after 48 hrs	[PMID: 16777409]
NCI-H460	IC₅₀	>100 μM Compound: tirapazamine	Cytotoxicity against human H460 cells under normoxic condition after 2 hrs by Alamar blue staining assay Cytotoxicity against human H460 cells under normoxic condition after 2 hrs by Alamar blue staining assay	[PMID: 18257544]
NCI-H460	IC₅₀	11 μM Compound: tirapazamine	Cytotoxicity against human H460 cells under hypoxic condition after 2 hrs by Alamar blue staining assay Cytotoxicity against human H460 cells under hypoxic condition after 2 hrs by Alamar blue staining assay	[PMID: 18257544]
NRK	EC₅₀	>100 μM Compound: 10; TPZ	Cytotoxicity against rat NRK cells assessed as reduction in cell viability incubated for 24 hrs under 19% O2 condition by Hoechst 33342 staining based microscopic analysis Cytotoxicity against rat NRK cells assessed as reduction in cell viability incubated for 24 hrs under 19% O2 condition by Hoechst 33342 staining based microscopic analysis	[PMID: 34124675]
NRK	EC₅₀	35 μM Compound: 10; TPZ	Cytotoxicity against rat NRK cells assessed as reduction in cell viability incubated for 24 hrs under 2% O2 condition by Hoechst 33342 staining based microscopic analysis Cytotoxicity against rat NRK cells assessed as reduction in cell viability incubated for 24 hrs under 2% O2 condition by Hoechst 33342 staining based microscopic analysis	[PMID: 34124675]
PC-3	IC₅₀	1.17 μM Compound: TPZ	Cytotoxicity against human PC3 cells for 72 hrs under hypoxic condition by MTT assay Cytotoxicity against human PC3 cells for 72 hrs under hypoxic condition by MTT assay	[PMID: 21281992]
PC-3	IC₅₀	20.97 μM Compound: TPZ	Cytotoxicity against human PC3 cells for 72 hrs under normoxic condition by MTT assay Cytotoxicity against human PC3 cells for 72 hrs under normoxic condition by MTT assay	[PMID: 21281992]
PC-3	IC₅₀	22.3 μM Compound: TPZ	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay Cytotoxicity against human PC3 cells after 48 hrs by MTT assay	[PMID: 16777409]
SCC-7	IC₅₀	2.4 μM Compound: 1	Inhibitory concentration against murine SCCVII cell line under hypoxic condition Inhibitory concentration against murine SCCVII cell line under hypoxic condition	[PMID: 12502371]
SCC-7	IC₅₀	71.7 μM Compound: 1	Inhibitory concentration against murine SCCVII cell line under aerobic condition Inhibitory concentration against murine SCCVII cell line under aerobic condition	[PMID: 12502371]
SiHa	IC₅₀	2.5 μM Compound: 1, TPZ	Cytotoxicity against human SiHa cells under hypoxic conditions after 4 hrs Cytotoxicity against human SiHa cells under hypoxic conditions after 4 hrs	[PMID: 18001018]
SiHa	IC₅₀	2.5 μM Compound: 1, TPZ	Cytotoxicity against human SiHa cells after 4 hrs under strict hypoxic condition Cytotoxicity against human SiHa cells after 4 hrs under strict hypoxic condition	[PMID: 18847185]
SMMC-7721	IC₅₀	32.79 μM Compound: TPZ	Cytotoxicity against human SMMC7721 cells for 72 hrs under normoxic condition by MTT assay Cytotoxicity against human SMMC7721 cells for 72 hrs under normoxic condition by MTT assay	[PMID: 21281992]
SMMC-7721	IC₅₀	4.75 μM Compound: TPZ	Cytotoxicity against human SMMC7721 cells for 72 hrs under hypoxic condition by MTT assay Cytotoxicity against human SMMC7721 cells for 72 hrs under hypoxic condition by MTT assay	[PMID: 21281992]
SW-620	IC₅₀	1.2 μM Compound: Tirapazamine	Cytotoxicity against human SW620 cells incubated for 4 hrs under hypoxic condition followed by compound washout and measured after 5 days by SRB assay Cytotoxicity against human SW620 cells incubated for 4 hrs under hypoxic condition followed by compound washout and measured after 5 days by SRB assay	[PMID: 30885680]
SW-620	IC₅₀	91.03 μM Compound: Tirapazamine	Cytotoxicity against human SW620 cells incubated for 4 hrs under aerobic condition followed by compound washout and measured after 5 days by SRB assay Cytotoxicity against human SW620 cells incubated for 4 hrs under aerobic condition followed by compound washout and measured after 5 days by SRB assay	[PMID: 30885680]
U-251	IC₅₀	71.2 μg/mL Compound: TPZ	Growth inhibition of human U251 cells after 48 hrs by SRB assay Growth inhibition of human U251 cells after 48 hrs by SRB assay	[PMID: 20236735]
Vero	CC₅₀	8 μg/mL Compound: TPZ	Cytotoxicity against african green monkey Vero cells after 72 hrs by CellTiterGlo assay Cytotoxicity against african green monkey Vero cells after 72 hrs by CellTiterGlo assay	[PMID: 22691154]

In Vitro

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

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

Cell Viability Assay^[1]

Cell Line:

SCC7 cells
Concentration:

1mg
Incubation Time:

24 h
Result:

Showed synergism with Pba at ED50, ED90 and ED95.

In Vivo

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].
.

MedChemExpress (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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 27314-97-2
Appearance Solid
Molecular Weight 178.15
Formula C₇H₆N₄O₂
Color Orange to red
SMILES

NC1=[N+]([O-])C2=CC=CC=C2[N+]([O-])=N1
Synonyms

SR259075; SR4233; Win59075; SML 0552; SR 259075; Tirazone
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (15)

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Adv Sci (Weinh)

Photo-Empowered Macrophage-Based Drug Delivery System Overcomes Motility Suppression and Significantly Enhances Deep Tumor Drug Delivery. [Abstract]

2025 Nov 9:e15349. PMID: 41208150
Biomaterials

Microenvironment-activatable nanoagent for real-time NIR-II monitoring and targeted therapy of arterial restenosis. [Abstract]

2025 Jun 7:324:123482. PMID: 40499225
Biomaterials

Biomimetic cell membrane-coated glucose/oxygen-exhausting nanoreactor for remodeling tumor microenvironment in targeted hypoxic tumor therapy. [Abstract]

2022 Nov:290:121821. PMID: 36201949
J Nanobiotechnology

AMFR-mediated ER-phagy regulation and therapeutic targeting in osteosarcoma: a multifunctional nanoplatform strategy. [Abstract]

2025 Nov 18;23(1):717. PMID: 41250206
J Nanobiotechnology

Sonodynamic and sonomechanical effect on cellular stemness and extracellular physicochemical environment to potentiate chemotherapy. [Abstract]

2024 Jun 21;22(1):358. PMID: 38907270
J Control Release

Engineered biomimetic nanoreactor for synergistic photodynamic-chemotherapy against hypoxic tumor. [Abstract]

2022 Sep 22;351:151-163. PMID: 36122895
Acta Biomater

A Supramolecular Assembly Strategy for Hydrophilic Drug Delivery towards Synergistic Cancer Treatment. [Abstract]

2023 Jul 1:164:407-421. PMID: 37088157
Int J Biol Macromol

Dual modified ferritin nanocages for tumor-targeted and microenvironment-responsive drug delivery. [Abstract]

2025 Feb 4:140694. PMID: 39914543
Biomater Adv

Near-infrared photoactivatable three-in-one nanoagents to aggravate hypoxia and enable amplified photo-chemotherapy. [Abstract]

2024 Jul 19:163:213962. PMID: 39032435
Front Bioeng Biotechnol

Biomimetic Metal-Organic Framework Nanoparticles for Synergistic Combining of SDT-Chemotherapy Induce Pyroptosis in Gastric Cancer. [Abstract]

2022 Feb 21;10:796820. PMID: 35265591
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Nanotechnology

Hyaluronan-fullerene/AIEgen nanogel as CD44-targeted delivery of tirapazamine for synergistic photodynamic-hypoxia activated therapy. [Abstract]

2021 Aug 23;32(46). PMID: 34325415
J Antibiot (Tokyo)

Repurposing Tirazone as an effective quorum-sensing inhibitor against Pseudomonas aeruginosa virulence and biofilm formation. [Abstract]

2026 Apr;79(4):248-263. PMID: 41708876
Anal Biochem

In situ label-free and sensitive detection assay for cell apoptosis via polyadenosine-coralyne fluorescence enhancement strategy. [Abstract]

2021 Nov 1:632:114329. PMID: 34525387
Research Square Preprint

2021 Aug.

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (350.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

5.6132 mL

28.0662 mL

56.1325 mL

5 mM

1.1226 mL

5.6132 mL

11.2265 mL

10 mM

0.5613 mL

2.8066 mL

5.6132 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (14.03 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (56.13 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Cai TY, et al. Tirapazamine sensitizes hepatocellular carcinoma cells to topoisomerase I inhibitors via cooperative modulation of hypoxia-inducible factor-1α. Mol Cancer Ther. 2014 Mar;13(3):630-42. [Content Brief]

[2]. Sliwinska J, et al. Tirapazamine-doxorubicin interaction referring to heart oxidative stress and Ca2? balance protein levels. Oxid Med Cell Longev. 2012;2012:890826. [Content Brief]

[3]. 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. [Content Brief]

[4]. Romero, José, et al. Electronic structure and reactivity of tirapazamine as a radiosensitizer. Journal of molecular modeling vol. 27,6 177. 22 May. 2021. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	5.6132 mL	28.0662 mL	56.1325 mL	140.3312 mL
	5 mM	1.1226 mL	5.6132 mL	11.2265 mL	28.0662 mL
	10 mM	0.5613 mL	2.8066 mL	5.6132 mL	14.0331 mL
	15 mM	0.3742 mL	1.8711 mL	3.7422 mL	9.3554 mL
	20 mM	0.2807 mL	1.4033 mL	2.8066 mL	7.0166 mL
	25 mM	0.2245 mL	1.1226 mL	2.2453 mL	5.6132 mL
	30 mM	0.1871 mL	0.9355 mL	1.8711 mL	4.6777 mL
	40 mM	0.1403 mL	0.7017 mL	1.4033 mL	3.5083 mL
	50 mM	0.1123 mL	0.5613 mL	1.1226 mL	2.8066 mL
	60 mM	0.0936 mL	0.4678 mL	0.9355 mL	2.3389 mL
	80 mM	0.0702 mL	0.3508 mL	0.7017 mL	1.7541 mL
	100 mM	0.0561 mL	0.2807 mL	0.5613 mL	1.4033 mL

Tirapazamine

15 Cited Publications

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Tirapazamine

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

FDA Approved & Pharmacopeial Drug Library

Rare Diseases Drug Library

Highly Selective Inhibitors Library

Radiosensitizer Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Tirapazamine

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Publications (15)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tirapazamine

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

FDA Approved & Pharmacopeial Drug Library

Rare Diseases Drug Library

Highly Selective Inhibitors Library

Radiosensitizer Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Tirapazamine

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Publications (15)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tirapazamine Related Classifications

Cat. No.: HY-13767