Misonidazole
(Synonyms: 米索硝唑,NSC 261037,Ro 7-0582,SR 1354) 目录号 : GC16331A nitroimidazole that targets hypoxic cells
Cas No.:13551-87-6
Sample solution is provided at 25 µL, 10mM.
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Misonidazole (MISO), a hypoxic cell radiosensitizer, is selectively metabolized by hypoxic cells to reactive products that bind covalently to cellular constituents. The drug also possesses a substantial cytotoxic effect, independent of radiation, which is selectively expressed in hypoxic cells. Misonidazole may be cytotoxic to the normal hypoxic tissues in the human body, making this became a major concern in the clinical application of the drug. Misonidazole leads to strand breaks in cellular DNA and those cells which fail to survive also fail to repair these strand breaks. Misonidazole depletes intracellular glutathione and is more toxic in glutathione depleted cells. The depletion is time, temperature, drug concentration and cell line dependent.
In vitro: In cultured CHO cells, pretreatment with 5 mM MISO for 2 hr exihibited the marginal toxicity [2].
In vivo: Pretreatment with misonidazole (MISO) enhanced the number of cross-links formed in a fibrosarcoma and in the spleen and gut of mice for periods up to 48 h following a single injection of melphalan (MEL). MISO pretreatment could result in a greater amount of binding of MEL to DNA at early times after injection. MISO may exert its affect by inhibiting the repair of cross-links or monoadducts at early times post-injection [3].
Clinical trials: Various dose schedules of misonidazole have proven to be tolerable, with a moderate incidence of nausea and vomiting and mild peripheral neuropathy, and a low incidence of more severe peripheral neuropathy or central neuropathy [4].
References:
[1] Josephy P D, Palcic B, Skarsgard L D. Ascorbate-enhanced cytotoxicity of misonidazole[J]. Nature, 1978, 271(5643): 370-372.
[2]Taylor Y C, Bump E A, Brown J M. Studies on the mechanism of chemosensitization by misonidazole in vitro[J]. International Journal of Radiation Oncology Biology Physics, 1982, 8(3-4): 705-708.
[3] Murray D, Meyn R E. Enhancement of the DNA cross-linking activity of melphalan by misonidazole in vivo[J]. British journal of cancer, 1983, 47(2): 195.
[4] Wasserman T H, Stetz J A, Phillips T L. Clinical trials of misonidazole in the United States[J]. Cancer clinical trials, 1980, 4(1): 7-16.
| Cas No. | 13551-87-6 | SDF | |
| 别名 | 米索硝唑,NSC 261037,Ro 7-0582,SR 1354 | ||
| 化学名 | α-(methoxymethyl)-2-nitro-1H-imidazole-1-ethanol | ||
| Canonical SMILES | OC(COC)CN1C=CN=C1[N+]([O-])=O | ||
| 分子式 | C7H11N3O4 | 分子量 | 201.2 |
| 溶解度 | ≤5mg/ml in ethanol;15mg/ml in DMSO;15mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.9702 mL | 24.8509 mL | 49.7018 mL |
| 5 mM | 0.994 mL | 4.9702 mL | 9.9404 mL |
| 10 mM | 0.497 mL | 2.4851 mL | 4.9702 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet