(±)-10-Hydroxycamptothecin
(Synonyms: 10-羟基喜树碱,(±)-10-HCPT) 目录号 : GC38194
Hydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.
Cas No.:64439-81-2
Sample solution is provided at 25 µL, 10mM.
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Hydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.
10-HCPT has an inhibitory effect on phosphorylation of histone H1 and H3 in murine hepatoma cells and also exhibits a differentiation inducing effect in human HepG2 cells. 10-HCPT inhibits the cell growth, reduces the cell viability and disturbs the cell cycle distribution of human colon cancer cell line Colo 205. It induces cell cycle arrest in the G2/M phase[1].
10-HCPT can be safely orally administered and, alternatively, a low-dose long-term treatment[1]. Prolonged elimination of HCPT in vivo may have a significant impact on its therapeutic effects. HCPT is metabolized to its carboxylate form and glucuronides. Dose-dependent toxicity is observed with i.v. administration of HCPT[2].
[1] Ping YH, et al. Oncol Rep. 2006, 15(5):1273-9. [2] Zhang R, et al. Cancer Chemother Pharmacol. 1998, 41(4):257-67.
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Cell experiment: |
Colo 205 cells (5 × 105) (ATCC: CCL-222) are seeded in 25T flasks overnight and then treated without (control) and with 5, 10, 15 or 20 nM of (±)-10-Hydroxycamptothecin, respectively. After treatment for 24-120 h, cells are harvested by trypsin-EDTA and then centrifuged at 1,500 rpm for 5 min at 4˚C. The cell pellet is resuspended in culture medium containing 0.04% trypan blue and the viable cells are enumerated by a hemocytometer[2]. |
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Animal experiment: |
BALB/c-nu mice are housed in a laminar flow room under sterilized conditions with a maintained temperature of 25 ± 2˚C and a controlled 12-h light and 12-h dark cycle. The Colo 205 cells are harvested and resuspended in serum-free RPMI-1640 medium. Cells are adjusted to 1 × 107 cells/mL, and transplanted 0.1 mL subcutaneously to the flank regions of the mice. Each experimental group included six to seven mice bearing tumors. (±)-10-Hydroxycamptothecin is dissolved in propylene glycol and treatment begins when the tumor size reach 3-5 mm. (±)-10-Hydroxycamptothecin is administered via p.o. once per two or four days at doses of 1, 2.5, 5, 7.5 mg/kg (volume of injection: 0.1 mL/20 g of body weight), respectively. The control group receives propylene glycol vehicle once per two days. Tumor size and body weight are monitored twice a week throughout the experiment. The tumor size is measured using a vernier caliper. Tumor volume (V) is calculated according to the formula: V (mm3) = 0.4AB2, where A and B are the longest diameter and the shortest diameter, respectively. At the end of the experiment, all mice are sacrificed by CO2 gas. Tumors, livers, kidneys and lungs are collected, fixed, embedded and stained with hematoxylin and eosin for pathological analysis[2]. |
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References: [1]. Liu SY, et al. Interaction of several nucleoside triphosphate analogues and 10-hydroxycamptothecin with human DNA topoisomerases. Cancer Res. 1989 Mar 15;49(6):1366-70. |
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| Cas No. | 64439-81-2 | SDF | |
| 别名 | 10-羟基喜树碱,(±)-10-HCPT | ||
| Canonical SMILES | O=C1C(O)(CC)C2=C(CO1)C(N3CC4=CC5=CC(O)=CC=C5N=C4C3=C2)=O | ||
| 分子式 | C20H16N2O5 | 分子量 | 364.35 |
| 溶解度 | DMSO: ≥ 37.5 mg/mL (102.92 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 | 2.7446 mL | 13.7231 mL | 27.4461 mL |
| 5 mM | 0.5489 mL | 2.7446 mL | 5.4892 mL |
| 10 mM | 0.2745 mL | 1.3723 mL | 2.7446 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet