Mithramycin A
(Synonyms: 光辉霉素,Mithramycin A) 目录号 : GC15060A DNA-binding antitumor antibiotic
Cas No.:18378-89-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment: |
HEp-2 cells and KB cells are cultured in DMEM 100 U/mL each of Penicillin and Streptomycin and 10% FBS for HEp-2 cells and 5% FBS for KB in a humidified atmosphere containing 5% CO2 at 37°C. Equal numbers of cells are seeded and allowed to attach. At 50-60% confluence, cells are treated with DMSO or indicated concentrations of Plicamycin (50, 100, and 200 nM for HEp-2 cells; 20, 40, and 80 nM for KB cells). Cell viability is determined using CellTiter 96 Aqueous One Solution Cell Proliferation Assay Kits. In brief, cells are seeded in 96-well plates and incubated with Plicamycin. After treatment, 30 µL MTS solution is added to each well and cells are incubated for 2 h at 37°C. MTS solution is analyzed using a microplate reader at 490 nm and 690 nm[1]. |
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Animal experiment: |
Mice[1]Female nude mice are used. KB cells are suspended in sterile PBS and injected subcutaneously into the right flank of mice. Mice are randomized into two groups containing five mice each and treated with 0.2 mg/kg/day of Plicamycin (i.p.) three times per week for 29 days. Control mice receive an equal volume of vehicle. After 29 days, bodies, organs and tumors are weighed and tumor volumes determined. Tumors are measured[1]. |
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References: [1]. Choi ES, et al. Modulation of specificity protein 1 by mithramycin A as a novel therapeutic strategy for cervical cancer. Sci Rep. 2014 Nov 24;4:7162. |
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Plicamycin is a selective specificity protein 1 (Sp1) inhibitor. Plicamycin inhibits the growth of various cancers by decreasing Sp1 protein.
Sp1 is a zinc-finger transcription factor that regulates multiple cellular functions and promotes tumor progression by controlling expression of genes involved in cell cycle, apoptosis and DNA damage. Sp1 binds to GC-rich motifs of promoters and interacts with components of the general transcriptional machinery and co-activator complexes of multiple signaling pathways. Plicamycin (Mith) decreases Sp1 protein by inducing proteasome-dependent degradation, thereby suppressing cervical cancer growth through a DR5/caspase-8/Bid signaling pathway. To assess the antiproliferative effects of Plicamycin on cervical cancer cells, two cervical cancer cell lines with different genetic backgrounds are grown with or without treatment with Plicamycin at different concentrations. Plicamycin inhibits HEp-2 and KB cell growth in a concentration-dependent manner after 48 h. Apoptotic cell death is qualitatively estimated by DAPI staining for nuclear condensation and fragmentation. Plicamycin leads to significant DNA fragmentation compared to untreated controls[1].
The antitumorigenic activity of Plicamycin (0.2 mg/kg/day) is determined in a xenograft model and observed reduction in tumor volume and weight. No significant mouse body weight loss is observed in Plicamycin-treatment groups, indicating that Plicamycin-associated toxicity is minimal. Plicamycin also increases TUNEL-positive cells in tumor xenografts. No notable intergroup differences are observed among organs, indicating no marked signs of systemic toxicity at the Plicamycin dose used in this study[1].
References:
[1]. Choi ES, et al. Modulation of specificity protein 1 by mithramycin A as a novel therapeutic strategy for cervical cancer. Sci Rep. 2014 Nov 24;4:7162.
| Cas No. | 18378-89-7 | SDF | |
| 别名 | 光辉霉素,Mithramycin A | ||
| 化学名 | (1S)-5-Deoxy-1-C-[(2S,3S)-7-[[2,6-dideoxy-3-O-(2,6-dideoxy--D-arabino-hexopyranosyl)--D-arabino-hexopyranosyl]oxy]-3-[(O-2,6-dideoxy-3-C-methyl--D-ribo-hexopyranosyl-(1.fwdarw.3)-O-2,6-dideoxy--D-lyxo-hexopyranosyl-(1.fwdarw.3)-2,6-dideoxy--D-arabino-hexo | ||
| Canonical SMILES | CC1C(C(CC(O1)OC2CC(OC(C2O)C)OC3=CC4=CC5=C(C(=O)C(C(C5)C(C(=O)C(C(C)O)O)OC)OC6CC(C(C(O6)C)O)OC7CC(C(C(O7)C)O)OC8CC(C(C(O8)C)O)(C)O)C(=C4C(=C3C)O)O)O)O | ||
| 分子式 | C52H76O24 | 分子量 | 1085.16 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 2 mg/ml | 储存条件 | Desiccate 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 | 0.9215 mL | 4.6076 mL | 9.2152 mL |
| 5 mM | 0.1843 mL | 0.9215 mL | 1.843 mL |
| 10 mM | 0.0922 mL | 0.4608 mL | 0.9215 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。