Camptothecin-20(S)-O-propionate
(Synonyms: Camptothecin-20-O-propionate) 目录号 : GC60669
Camptothecin-20(S)-O-propionate(CZ48)是喜树碱(CPT)的类似物，是强效的抗肿瘤化合物。Camptothecin-20(S)-O-propionate(CZ48)是拓扑异构酶I(topoisomerase-Ι)的抑制剂。
Cas No.:194414-69-2
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
Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor[1][2][3].
Camptothecin-20(S)-O-propionate (CZ48, gavage, 100 to 2000 mg/kg/day) exhibits anti-tumor activity in CLO-breast carcinoma (100 mg/kg) and PC3-prostate carcinoma (1000 mg/kg) models in mice[3]. Animal Model: A tumor xenograft growing in a nude mouse (size, ∼1 cm3)[3].
[1]. Zhisong Cao, et al. Crystalline camptothecin-20(S)-O-propionate hydrate: a novel anticancer agent with strong activity against 19 human tumor xenografts. Cancer Res. 2009 Jun 1;69(11):4742-9. [2]. Zhisong Cao, et al. Crystalline camptothecin-20(S)-O-propionate hydrate: a novel anticancer agent with strong activity against 19 human tumor xenografts. Cancer Res. 2009 Jun 1;69(11):4742-9. [3]. Xing Liu, et al. Correlation between the sensitivity of tumors to treatment with CZ48 and local concentrations of the active metabolite CPT within the tumors. Biomed Rep. 2013 Mar;1(2):202-206.
| Cas No. | 194414-69-2 | SDF | |
| 别名 | Camptothecin-20-O-propionate | ||
| Canonical SMILES | O=C1[C@](CC)(C2=C(C(N3CC4=CC5=CC=CC=C5N=C4C3=C2)=O)CO1)OC(CC)=O | ||
| 分子式 | C23H20N2O5 | 分子量 | 404.42 |
| 溶解度 | DMSO: 9.09 mg/mL (22.48 mM) | 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 | 2.4727 mL | 12.3634 mL | 24.7268 mL |
| 5 mM | 0.4945 mL | 2.4727 mL | 4.9454 mL |
| 10 mM | 0.2473 mL | 1.2363 mL | 2.4727 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。
Crystalline Camptothecin-20(S)-O-propionate hydrate: a novel anticancer agent with strong activity against 19 human tumor xenografts
Cancer Res 2009 Jun 1;69(11):4742-9.PMID:19458069DOI:10.1158/0008-5472.CAN-08-4452
To find a more effective and less toxic chemotherapeutic agent, we have successfully prepared crystalline Camptothecin-20(S)-O-propionate hydrate (CZ48) by reacting camptothecin with propionic anhydride using concentrated sulfuric acid as catalyst. The biological effectiveness of this new anticancer agent was evaluated by using xenografts of human cancers in nude mice as the testing models. The extensive treatment of 21 human tumors with various dose levels of CZ48 has shown that this agent is highly effective against many different human tumors tested with a striking lack of toxicity. Of the 21 human tumor lines tested, 9 regressed, 5 were <10% of the control, 3 were <20%, and 2 were <40%. Two tumors did not respond. The total response rate was 90% (19 of 21). No toxicity was observed in mice. The effective doses required to achieve the positive response varied from 100 to 1,000 mg/kg/d depending on the tumors. The maximum tolerated dose was not reached because of the nontoxic nature of the drug in mice. Thus, this compound has a much wider therapeutic index compared with that of the existing anticancer drugs currently in use.