Duocarmycin Analog
目录号 : GC38080
Duocarmycin Analog 是 Duocarmycin 的类似物，可用作 DNA 烷化剂 (DNA alkylator) 和 抗体-药物偶联物 (ADC cytotoxin) 的毒素部分。
Cas No.:372954-15-9
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
Duocarmycin Analog is an analog of Duocarmycin, and used as an DNA alkylator and ADC cytotoxin[1].
[1]. Boger, Dale L. CBI ANALOGUES OF CC-1065 AND THE DUOCARMYCINS. WO2003022806A2
| Cas No. | 372954-15-9 | SDF | |
| Canonical SMILES | O=C(OC(C)(C)C)NC1=CC=C(C(NC2=CC3=C(NC(C(N4C[C@@H](CCl)C5=C4C=C(O)C6=CC=CC=C56)=O)=C3)C=C2)=O)C=C1 | ||
| 分子式 | C34H31ClN4O5 | 分子量 | 611.09 |
| 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 | 1.6364 mL | 8.1821 mL | 16.3642 mL |
| 5 mM | 0.3273 mL | 1.6364 mL | 3.2728 mL |
| 10 mM | 0.1636 mL | 0.8182 mL | 1.6364 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, nuclear localization, and biological activity of a fluorescent Duocarmycin Analog, HxTfA
Bioorg Med Chem Lett 2018 May 1;28(8):1342-1347.PMID:29548574DOI:10.1016/j.bmcl.2018.03.016.
HxTfA 4 is a fluorescent analog of a potent cytotoxic and antimalarial agent, TfA 3, which is currently being investigated for the development of an antimalarial vaccine, PlasProtect®. HxTfA contains a p-anisylbenzimidazole or Hx moiety, which is endowed with a blue emission upon excitation at 318 nm; thus enabling it to be used as a surrogate for probing the cellular fate of TfA using confocal microscopy, and addressing the question of nuclear localization. HxTfA exhibits similar selectivity to TfA for A-tract sequences of DNA, alkylating adenine-N3, albeit at 10-fold higher concentrations. It also possesses in vitro cytotoxicity against A549 human lung carcinoma cells and Plasmodium falciparum. Confocal microscopy studies showed for the first time that HxTfA, and by inference TfA, entered A549 cells and localized in the nucleus to exert its biological activity. At biologically relevant concentrations, HxTfA elicits DNA damage response as evidenced by a marked increase in the levels of γH2AX observed by confocal microscopy and immunoblotting studies, and ultimately induces apoptosis.