Doranidazole
Doranidazole (PR 350) is a radiosensitizer. Doranidazole increases the radiosensitivity of hypoxic SCCVII cells. Doranidazole significantly enhances radiation-induced growth delay in SCCVII tumors when administered intravenously before tumor irradiation. Doranidazole radiosensitizes tumors to an extent that depends on the tumor's oxygenation status. Doranidazole can be used for the study of lymphoma and hypoxic pancreatic tumors.
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- CAS No.: 149838-23-3
- Formule: C8H13N3O6
- Masse moléculaire:247.21
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
In Vitro
Doranidazole (1 mM) significantly enhances the radiosensitivity of hypoxic SCCVII cells in vitro[1].
Doranidazole (0.1-3.0 mM) can dose-dependently increase radiation-induced micronucleus formation in hypoxic SCCVII cells[1].
Doranidazole (1 mM) enhances radiation-induced apoptosis in Mouse L5178Y lymphoma cells under hypoxic conditions[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Doranidazole (50-200 mg/kg, tail vein injection, once) significantly enhances radiation-induced growth delay of SCCVII tumors in mice and reduces the radiation dose required[1].
Doranidazole (200 mg/kg, tail vein injection, once) can enhance the radiosensitization response of CFPAC-1 tumors in nude mice, but has no radiosensitizing effect on MIA PaCa-2 tumors[1].
Doranidazole (50-200 mg/kg, tail vein injection, once) exhibits a radiosensitizing effect that correlates with tumor oxygenation status; tumors with high hypoxia (such as SCCVII and CFPAC-1) respond better, while well-oxygenated tumors (such as MIA PaCa-2) show no sensitizing effect[1].
Doranidazole (100-250 mg/kg, i.v., once) shows a clear radiosensitizing effect on all four pancreatic cancer cell lines in xenograft nude mice, and the effect is dose-dependent[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C3H/HeN mice were subcutaneously inoculated with SCCVII cells (approximately 2 × 106 cells) in the right hind leg[1].
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Dosage:50 mg/kg, 100 mg/kg, 200 mg/kg
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Administration:Tail vein injection, once
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Result:The SERs were 1.09-1.36 at 10 min after 50-200 mg/kg injection, indicating caused significant radiosensitization of tumors within 10 min after the drug administration.
The maximum radiosensitization of tumor with a SER of 1.47 occurred 20 min after administration at 200 mg/kg.
Considerable radiosensitization was still evident 40 min after drug administration.
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Animal Model:Female C3H/HeN mice were subcutaneously inoculated with SCCVII cells (approximately 2 × 106 cells) in the right hind leg[1].
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Dosage:50 mg/kg, 100 mg/kg, 200 mg/kg
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Administration:Tail vein injection, once
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Result:An administration of 200 mg/kg alone exerted no effect on the growth of SCCVII tumors.
100 mg/kg was slightly slower than that of the tumors irradiated after saline injection.
The radiation-induced growth delay was further enhanced with 200 mg/kg.
Combining 200 mg/kg with irradiation extended the tumor doubling time to 36 days.
Reduce the required radiation dose.
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Animal Model:BALB/c-nu/nu nude mice were subcutaneously inoculated with Human pancreatic tumor cells (CFPAC-1 and MIA Paca-2) in the right hind leg (approximately 5 × 106 cells were inoculated first, and after the tumor grew to 1 cm in diameter, it was cut into small pieces and transplanted into new mice to ensure that the tumors were of uniform size)[1].
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Dosage:200 mg/kg
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Administration:Tail vein injection, once
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Result:Combined irradiation prolonged the regeneration time of CFPAC-1 tumors to 91 days.
No significant difference in tumor growth delay between the combined irradiation group and the irradiation-alone group in MIA PaCa-2 tumors, which may be related to the better oxygenation status of these tumors.
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Animal Model:Four human pancreatic cancer cell lines (SUIT-2, PANC-1, MIA PaCa-2, and BxPC-3) in their exponential growth phase were subcutaneously inoculated at 106 cells per cell in the back of 6-week-old male Balb/c nude mice[3].
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Dosage:100 mg/kg, 250 mg/kg
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Administration:I.v., once
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Result:At a dose of 100 mg/kg, the SER was 1.15–1.3 (SUIT-2: 1.15, PANC-1: 1.3, MIA PaCa-2: 1.2, BxPC-3: 1.25).
At a dose of 250 mg/kg, the SER increased to 1.35–1.45 (SUIT-2: 1.35, PANC-1: 1.45, MIA PaCa-2: 1.4, BxPC-3: 1.35).
Chemical Information
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CAS No. 149838-23-3
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Masse moléculaire 247.21
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Formule C8H13N3O6
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SMILES
OC[C@H](O)[C@@H](CO)OCN1C([N+]([O-])=O)=NC=C1
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Synonyms
PR 350; RP 343
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Yahiro T, et al. Effects of hypoxic cell radiosensitizer doranidazole (PR-350) on the radioresponse of murine and human tumor cells in vitro and in vivo. J Radiat Res. 2005 Sep;46(3):363-72. [Content Brief]
[3]. Shibamoto Y, et al. Radiosensitivity of human pancreatic cancer cells in vitro and in vivo, and the effect of a new hypoxic cell sensitizer, doranidazole. Radiother Oncol. 2000 Aug;56(2):265-70. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Doranidazole Related Classifications
HY-105095 Related Classifications
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