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Doranidazole (PR 350) 是一种放射增敏剂。Doranidazole 可提高乏氧 SCCVII 细胞的放射敏感性。在肿瘤照射前静脉注射 Doranidazole 可显著增强放射诱导的 SCCVII 肿瘤生长延迟。Doranidazole 对肿瘤的放射敏感性增强程度取决于肿瘤的氧合状态。Doranidazole 可用于淋巴瘤和乏氧胰腺肿瘤的研究。

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Doranidazole

Doranidazole Chemical Structure

CAS No. : 149838-23-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2][3].

体外研究
(In Vitro)

Doranidazole (1 mM) 可显著增强体外缺氧 SCCVII 细胞的放射敏感性[1]
Doranidazole (0.1-3.0 mM) 可剂量依赖性地增加缺氧 SCCVII 细胞中辐射诱导的微核形成[1]
Doranidazole (1 mM) 在缺氧条件下可增强小鼠 L5178Y 淋巴瘤细胞的辐射诱导凋亡[2]

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

体内研究
(In Vivo)

Doranidazole (50-200 mg/kg,尾静脉注射,单次) 可显著增强小鼠 SCCVII 肿瘤细胞的放射敏感性[1]
Doranidazole (50-200 mg/kg,尾静脉注射,单次) 可显著增强辐射诱导的小鼠 SCCVII 肿瘤生长延迟,并降低所需的辐射剂量[1]
Doranidazole (200 mg/kg,尾静脉注射,单次) 可增强裸鼠 CFPAC-1 肿瘤的放射增敏反应,但对 MIA PaCa-2 肿瘤无放射增敏作用[1]
Doranidazole (50-200 mg/kg,尾静脉注射,单次) 的放射增敏作用与肿瘤的氧合状态相关;高氧合肿瘤 (如 SCCVII 和 CFPAC-1) 的反应更佳,而氧合良好的肿瘤 (如 MIA PaCa-2) 则无增敏作用[1]
Doranidazole (100-250 mg/kg,静脉注射,单次) 对裸鼠异种移植模型中的所有四种胰腺癌细胞系均显示出明显的放射增敏作用,且该作用呈剂量依赖性[3]

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

Animal Model: Female C3H/HeN mice were subcutaneously inoculated with SCCVII cells (approximately 2 × 106 cells) in the right hind leg[1].
Dosage: 50 mg/kg, 100 mg/kg, 200 mg/kg
Administration: Tail vein injection, once
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.
Animal Model: Female C3H/HeN mice were subcutaneously inoculated with SCCVII cells (approximately 2 × 106 cells) in the right hind leg[1].
Dosage: 50 mg/kg, 100 mg/kg, 200 mg/kg
Administration: Tail vein injection, once
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.
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].
Dosage: 200 mg/kg
Administration: Tail vein injection, once
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.
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].
Dosage: 100 mg/kg, 250 mg/kg
Administration: I.v., once
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).
分子量

247.21

Formula

C8H13N3O6

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Doranidazole
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