Uramustine
目录号 : GC37860
Uramustine 是一种可口服的烷化剂 (alkylator)，可用于治疗淋巴肉瘤、慢性淋巴性白血病和血小板增多症。
Cas No.:66-75-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | The K562 human chronic myeloid leukemia cells are maintained in RPM1 1640 medium supplemented with 10% fetal calf serum and 2 mM glutamine at 37°C in a humidified atmosphere containing 5% CO2 and are incubated with a specified dose of drug for 1 h at 37°C in the dark. The incubation is terminated by centrifugation (5 min, 300 g), and the cells are washed once with drug-free medium. Following the appropriate Uramustine treatment, the cells are transferred to 96-well microtiter plates, with 104 cells per well and 8 wells per sample. Plates are then kept in the dark at 3°C in a humidified atmosphere containing 5% CO2. The assay is based on the ability of viable cells to reduce a yellow soluble tetrazolium salt, MTT to an insoluble purple formazan precipitate. Following incubation of the plates for 4 days (to allow control cells to increase in number by 10-fold), 20 μL of a 5 mg/mL solution of MTT in phosphate-buffered saline is added to each well and the plates are further incubated for 5 h. The plates are then centrifuged for 5 min at 300 g, and the bulk of the medium is pipetted from the cell pellet, leaving 10?20 μL per well. A total of 200 μL of DMSO is added to each well, and the samples are agitated to ensure complete mixing. The optical density is then read at a wavelength of 550 nm on a plate reader, and the dose?response curve is constructed. For each curve, an IC50 value is read as the dose required to reduce the final optical density to 50% of the control value[1]. |
References: [1]. Baraldi PG, et al. Design, synthesis, and biological activity of hybrid compounds between uramustine and DNA minor groove binder distamycin A. J Med Chem. 2002 Aug 15;45(17):3630-3638. | |
Uramustine is an oral alkylating agent, effective in the treatment of lymphosarcoma, chronic lymphatic leukaemia, and thrombocythemia. DNA Alkylator[1]
Uramustine is an oral alkylating agent, with potent antitumor activity. Uramustine inhibits human chronic myeloid leukaemia K562 cell line, with an IC50 of 5.1 μM.
[1]. Baraldi PG, et al. Design, synthesis, and biological activity of hybrid compounds between uramustine and DNA minor groove binder distamycin A. J Med Chem. 2002 Aug 15;45(17):3630-3638.
| Cas No. | 66-75-1 | SDF | |
| Canonical SMILES | O=C1NC(C(N(CCCl)CCCl)=CN1)=O | ||
| 分子式 | C8H11Cl2N3O2 | 分子量 | 252.1 |
| 溶解度 | Soluble in DMSO | 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 | 3.9667 mL | 19.8334 mL | 39.6668 mL |
| 5 mM | 0.7933 mL | 3.9667 mL | 7.9334 mL |
| 10 mM | 0.3967 mL | 1.9833 mL | 3.9667 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。
Design, synthesis, and biological activity of hybrid compounds between Uramustine and DNA minor groove binder distamycin A
J Med Chem 2002 Aug 15;45(17):3630-8.PMID:12166936DOI:10.1021/jm011113b.
The design, synthesis, characterization, DNA binding properties, and cytotoxic activity of a novel series of hybrids, namely, a molecular combination of the natural antibiotic distamycin A and the antineoplastic agent Uramustine, are reported, and the structure-activity relationships are discussed. This homologous series 29-34 consisted of the minor groove binder distamycin A joined to Uramustine (uracil mustard) by suitable aliphatic carboxylic acid moieties containing a flexible polymethylene chain that is variable in length [(CH(2))(n)(), where n = 1-6). All the hybrid compounds in this series exhibit enhanced activity compared to both distamycin A and Uramustine derivatives 22-27 used for conjugation, giving IC(50) values in the range 7.26-0.07 microM following a 1 h exposure of human leukemic K562 cells, with maximal activity shown when n = 6. The distance between the Uramustine and distamycin frame is crucial for the cytotoxicity, with compounds having linker lengths of four to six being at least 20-fold more cytotoxic than linker lengths one to three. Taq polymerase stop experiments demonstrated selective covalent binding of uramustine-distamycin hybrids to A/T rich DNA sequences, which was again more efficient with compounds 32-34 with a longer linker length. Two consequences can be derived from our study: (a) the distamycin moiety directs binding to the minor groove of A/T rich DNA sequences and, consequently, is responsible for the alkylation regioselectivity found in footprinting studies; (b) the higher flexibility due to a longer linker between the distamycin and uracil moieties allows the formation of complexes with the mustard moiety situated more deeply in the minor groove and, hence, with better alkylating properties.