Luzopeptin A
(Synonyms: BBM-928A) 目录号 : GC11740A DNA-intercalating antitumor agent
Cas No.:75580-37-9
Sample solution is provided at 25 µL, 10mM.
Luzopeptin A is a cyclic depsipeptide antibiotic.
A depsipeptide is a peptide in which one or more of its amide groups are replaced by the corresponding ester, or more generally, is a molecule that has both peptide and ester linkages in proximity in the same amino acid-containing small molecule or chain.
In vitro: Previous study found that luzopeptin A treatment could produce additional DNA bands which were the products of type II biintercalation. The types of restriction fragments involved were identified. Maximal type II biintercalation occurred at a luzopeptin A/DNA range of 0.14 to 0.18, at which more than 50% of the total DNA molecules were involved. Type II products were gradually converted to type I products upon prolonged incubation at 37 degrees, maybe due to the tendency for intermolecular bonds to disrupt. Echinomycin treatment failed to produce type II products, probably because of a DNA-binding affinity weaker than that of luzopeptin A [1].
In vivo: Animal study showed that when administered as a suspension in 0.9% NaCl solution, luzopeptin A demonstrated good activity against i.p. B16 melanoma and i.p. P388 leukemia and weak activity versus i.v. P388, i.p. L1210 leukemia, Lewis lung, and Madison 109 lung carcinomas. In terms of tumor cell kill, luzopeptin A induced net reductions in the body burdens of L1210 and P388 leukemias following single-drug injections but failed to yield net reductions following multiple-injection therapies [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Huang, C. H.,Mirabelli, C.K.,Mong, S., et al. Intermolecular cross-linking of DNA through bifunctional intercalation of an antitumor antibiotic, luzopeptin A (BBM-928A). Cancer Research 43, 2718-2724 (1983).
[2] Rose WC, Schurig JE, Huftalen JB, Bradner WT. Experimental antitumor activity and toxicity of a new chemotherapeutic agent, BBM 928A. Cancer Res. 1983 Apr;43(4):1504-10.
Cas No. | 75580-37-9 | SDF | |
别名 | BBM-928A | ||
化学名 | Luzopeptin A | ||
Canonical SMILES | CC(O[C@@H]1[C@@](N2N=CC1)([H])C(NCC(N(C)CC(N(C)[C@@H](C(O)(C)C)C(OC[C@@H](NC(C3=NC4=CC=C(OC)C=C4C=C3O)=O)C(N5[C@]([C@@H](OC(C)=O)CC=N5)([H])C(NCC(N(C)CC(N(C)[C@@H](C(O)(C)C)C(OC[C@@H](NC(C6=NC(C=CC(OC)=C7)=C7C=C6O)=O)C2=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)= | ||
分子式 | C64H78N14O24 | 分子量 | 1427.4 |
溶解度 | Soluble in DMSO;Soluble 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 0.7006 mL | 3.5029 mL | 7.0057 mL |
5 mM | 0.1401 mL | 0.7006 mL | 1.4011 mL |
10 mM | 0.0701 mL | 0.3503 mL | 0.7006 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet