产品名称

10-羟基喜树碱 (简称：10-HCPT)

10-Hydroxycamptothecin (Abbreviation: 10-HCPT)

化学名称

(S)-4-乙基-4,9-二羟基-1H-吡喃并[3',4':6,7]吲哚嗪并[1,2-b]喹啉-3,14(4H,12H)-二酮

(S)-4-Ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione

核心类别

喜树碱（Camptothecin）的天然衍生物，拓扑异构酶I（Topo I）抑制剂。

A natural derivative of Camptothecin, a Topoisomerase I (Topo I) inhibitor.

植物来源

最初从喜树 (Camptotheca acuminataDecne.) 的树皮和果实中分离得到。本产品主要通过半合成制得（以喜树碱为原料）。

Originally isolated from the bark and fruit of Camptotheca acuminata Decne. This product is primarily semisynthesized (using Camptothecin as raw material).

外观性状

淡黄色至黄色结晶性粉末，对光、热、湿敏感。

Pale yellow to yellow crystalline powder, sensitive to light, heat, and moisture.

主要规格

医药/科研级 (Pharma/Research Grade)：
- 纯度 (HPLC): ≥98.0%, ≥99.0%
- 单一杂质 (HPLC): ≤0.5%
- 水分 (Karl Fischer): ≤1.0%
- 有关物质 (Related Substances): ≤1.0%
中间体级 (Intermediate Grade)：
- 纯度 (HPLC): ≥95.0%

Pharmaceutical/Research Grade:
- Purity (HPLC): ≥98.0%, ≥99.0%
- Single Impurity (HPLC): ≤0.5%
- Water Content (Karl Fischer): ≤1.0%
- Related Substances: ≤1.0%
Intermediate Grade:
- Purity (HPLC): ≥95.0%

检测方法

HPLC, LC-MS, NMR, Karl Fischer

HPLC, LC-MS, NMR, Karl Fischer

CAS No.

19685-09-7

19685-09-7

分子式

C₂₀H₁₆N₂O₅

C₂₀H₁₆N₂O₅

分子量

364.35

364.35

药理功效

1. 拓扑异构酶I抑制剂 (Topo I Inhibitor)：核心机制。通过稳定Topo I-DNA共价复合物，阻碍DNA链的重新连接，导致DNA断裂和细胞死亡（凋亡），主要作用于S期细胞。
2. 广谱抗肿瘤 (Broad-spectrum Antitumor)：对多种实体瘤有效，包括肝癌、胃癌、结肠癌、卵巢癌、肺癌等。
3. 克服多药耐药性 (Overcomes Multidrug Resistance)：与许多化疗药物无交叉耐药性。
4. 水溶性改良前体 (Water-soluble Prodrug Precursor)：是合成水溶性喜树碱衍生物（如伊立替康、拓扑替康）的关键中间体。

1. Topo I Inhibitor: Core mechanism. By stabilizing the Topo I-DNA covalent complex, it hinders the religation of DNA strands, leading to DNA breaks and cell death (apoptosis), primarily affecting S-phase cells.
2. Broad-spectrum Antitumor: Effective against various solid tumors, including liver, gastric, colon, ovarian, and lung cancers.
3. Overcomes Multidrug Resistance: Exhibits no cross-resistance with many conventional chemotherapeutic agents.
4. Water-soluble Prodrug Precursor: A key intermediate for synthesizing water-soluble camptothecin derivatives (e.g., Irinotecan, Topotecan).

应用领域

医药研发：作为关键中间体，用于合成盐酸伊立替康、拓扑替康等前体药物；作为阳性对照品用于抗癌药物筛选。
临床研究：用于评估喜树碱类药物的药代动力学、药效学和毒性研究。
科学研究：作为工具化合物 (Tool Compound)，研究Topo I抑制剂的作用机制、肿瘤细胞凋亡通路、耐药性机制及新型衍生物的合成。

Pharmaceutical R&D: Used as a key intermediate for synthesizing prodrugs like Irinotecan Hydrochloride and Topotecan; serves as a positive control in anticancer drug screening.
Clinical Research: Used for evaluating the pharmacokinetics, pharmacodynamics, and toxicity of camptothecin-based drugs.
Scientific Research: Acts as a Tool Compound to investigate the mechanism of Topo I inhibitors, tumor cell apoptosis pathways, drug resistance mechanisms, and the synthesis of novel derivatives.

包装储存

关键提示：本品为细胞毒性物质 (Cytotoxic)，操作时需在通风橱内佩戴防护手套、口罩及护目镜。
包装：无菌玻璃瓶或氟化瓶（10mg, 50mg, 100mg, 1g, 5g）。
储存：密封，充氩或充氮保护，避光，2-8°C（冷藏） 或 -20°C（冷冻） 保存。严禁冻结（若含水）。保质期2年。

Critical Note: This product is a Cytotoxic substance. Operate in a fume hood wearing protective gloves, mask, and goggles.
Packaging: Sterile glass vials or fluorinated bottles (10mg, 50mg, 100mg, 1g, 5g).
Storage: Sealed, protected with Argon or Nitrogen, protected from light, store at 2-8°C (refrigerated) or -20°C (frozen). Do not freeze if aqueous. Shelf life 2 years.