Kazusamycin B
(Synonyms: CL 1957E, Hydroxyleptomycin A, PD 124895) 目录号 : GC43995
A bacterial metabolite
Cas No.:107140-30-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kazusamycin B is a bacterial metabolite originally isolated from Streptomyces. It has antifungal activity against S. pombe and R. javanicus (MICs = 0.05 and 2.13 µg/ml, respectively) but is inactive against Gram-positive and Gram-negative bacteria (MICs = >100 µg/ml). Kazusamycin B (5 ng/ml) halts the cell cycle at the G1 phase and induces nuclear condensation in L1210 cells, as well as inhibits nuclear-to-cytosolic transport of the HIV-1 regulatory protein Rev in HeLa cells expressing Rev (IC50 = 6.3 nM). It is cytotoxic to L1210 and HCT-8 cells with IC50 values of 1.8 and 1.6 ng/ml, respectively, and reduces tumor growth in a variety of murine tumor and mouse xenograft models.
| Cas No. | 107140-30-7 | SDF | |
| 别名 | CL 1957E, Hydroxyleptomycin A, PD 124895 | ||
| Canonical SMILES | O=C1OC(/C=C/C(C)=C\C(C)C/C=C/C(C)=C/C(CO)C(C(C)C(O)C(C)C/C(C)=C/C(O)=O)=O)C(C)C=C1 | ||
| 分子式 | C32H46O7 | 分子量 | 542.7 |
| 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 | 1.8426 mL | 9.2132 mL | 18.4264 mL |
| 5 mM | 0.3685 mL | 1.8426 mL | 3.6853 mL |
| 10 mM | 0.1843 mL | 0.9213 mL | 1.8426 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。
Kazusamycin B, a novel antitumor antibiotic
J Antibiot (Tokyo) 1987 Jun;40(6):778-85.PMID:3610834DOI:10.7164/antibiotics.40.778.
A novel antibiotic, Kazusamycin B (C32H46O7, MW 542), was isolated from the fermentation broth of Streptomyces sp. No. 81-484 and the structure was established mainly on the basis of its physico-chemical properties. Unambiguous 13C NMR spectral analysis of Kazusamycin B has been also accomplished. Kazusamycin B possesses potent cytocidal activities against L1210 (IC50 0.0018 micrograms/ml) and P388 (IC100 0.0016 micrograms/ml) leukemia cells in vitro.
The effect of Kazusamycin B on the cell cycle and morphology of cultured L1210 cells
J Antibiot (Tokyo) 1988 Dec;41(12):1854-61.PMID:3209477DOI:10.7164/antibiotics.41.1854.
The effect of a potent antitumor antibiotic, Kazusamycin B, on the cell cycle of L1210 cells was examined. Kazusamycin B arrested synchronized L1210 cells at G1 phase. Retardation of metaphase initiation was also observed. Flow cytometric analysis of kazusamycin B-treated asynchronized cells also confirmed G1 arresting effect of Kazusamycin B. In addition, an unidentified cell population with lower fluorescence intensity than G1 population was observed when the cells were exposed to the drug longer than 12 hours. Morphology of kazusamycin B-treated L1210 cells revealed that the intranuclear structure changed within 4 hours, and that abnormal condensation of nuclei coincided with the appearance of unidentified population. Kazusamycin B inhibited RNA synthesis moderately but specifically at 2 hours. However, this inhibition might be a secondary effect of the antibiotic-induced structural abnormality of the nuclei.
Antitumor effect of Kazusamycin B on experimental tumors
J Antibiot (Tokyo) 1987 Nov;40(11):1596-604.PMID:3693127DOI:10.7164/antibiotics.40.1596.
Kazusamycin B, a novel antibiotic (MW 542) isolated from fermentation broth of Streptomyces sp. No. 81-484 showed a broad antitumor spectrum both in vitro and in vivo. IC50 against the growth of tumor cells was around 1 ng/ml at 72 hours-exposure in vitro. Intraperitoneal injection of the antibiotic was effective in inhibiting the growth of murine tumors, S180, P388, EL-4, and B16. It was also active against doxorubicin-resistant P388, hepatic metastases of L5178Y-ML, pulmonary metastases of 3LL, and human mammary cancer MX-1 xenografted to nude mice. However, the activity of Kazusamycin B toward L1210 or human lung cancer LX-1 was weaker. According to the results of comparative studies on the effect of kazusamycins B and A, an analog of B, there seemed to be no significant difference in their effectiveness. The effective dose range and toxicity were markedly dependent on tumor lines tested and the regimen used. Maximum tolerated dose in mice with subcutaneous tumors was much higher than that in mice bearing ascitic leukemia as P388. Although intermittent administration could greatly reduce the cumulative toxicity of the drug, therapeutic effect was similar with both successive and intermittent administration schedules.