产品名称

7-乙基-10-羟基喜树碱 (简称：SN-38)

7-Ethyl-10-hydroxycamptothecin (Abbreviation: SN-38)

化学名称

(S)-4,11-二乙基-3,4,12,14-四羟基-3,14-二氧代-1H-吡喃并[3',4':6,7]吲哚嗪并[1,2-b]喹啉-9-酮

(S)-4,11-Diethyl-3,4,12,14-tetrahydroxy-3,14-dioxo-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-9-one

核心类别

喜树碱（Camptothecin）的活性代谢产物，拓扑异构酶I（Topo I）强效抑制剂。

The active metabolite of Camptothecin, a potent inhibitor of Topoisomerase I (Topo I).

植物来源

最初来源于喜树 (Camptotheca acuminataDecne.)，本产品主要通过半合成制得（以喜树碱或10-羟基喜树碱为原料）。

Originally derived from Camptotheca acuminata Decne., this product is primarily semisynthesized (using Camptothecin or 10-Hydroxycamptothecin as raw material).

外观性状

淡黄色至黄色结晶性粉末，对光、湿度敏感。

Pale yellow to yellow crystalline powder, sensitive to light 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%
- 细菌内毒素: <0.5 EU/mg (可选)
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%
- Bacterial Endotoxins: <0.5 EU/mg (Optional)
Intermediate Grade:
- Purity (HPLC): ≥95.0%

检测方法

HPLC, LC-MS, NMR, Karl Fischer

HPLC, LC-MS, NMR, Karl Fischer

CAS No.

86639-52-3

86639-52-3

分子式

C₂₂H₂₀N₂O₅

C₂₂H₂₀N₂O₅

分子量

392.41

392.41

药理功效

1. 强效拓扑异构酶I抑制剂 (Potent Topo I Inhibitor)：核心机制。SN-38是伊立替康（Irinotecan）在体内经羧酸酯酶活化后的主要活性代谢物，其抑制拓扑异构酶I的能力比喜树碱强100-1000倍。
2. 广谱强效抗肿瘤 (Broad-spectrum Potent Antitumor)：通过与拓扑异构酶I和DNA形成的三元复合物，阻断DNA复制和转录，诱导肿瘤细胞（尤其是S期细胞）凋亡。对结直肠癌、小细胞肺癌、胰腺癌等疗效显著。
3. 前药活化模型 (Prodrug Activation Model)：是研究前体药物（如伊立替康）活化机制和耐药性的关键分子。

1. Potent Topo I Inhibitor: Core mechanism. SN-38 is the primary active metabolite of Irinotecan (CPT-11) after activation by carboxylesterases in vivo. It is 100-1000 times more potent than Camptothecin in inhibiting Topoisomerase I.
2. Broad-spectrum Potent Antitumor: By forming a ternary complex with Topo I and DNA, it blocks DNA replication and transcription, inducing apoptosis in tumor cells (especially S-phase cells). Highly effective against colorectal cancer, small cell lung cancer, pancreatic cancer, etc.
3. Prodrug Activation Model: A key molecule for studying the activation mechanisms and drug resistance of prodrugs like Irinotecan.

应用领域

医药研发：作为关键中间体，用于合成或质控盐酸伊立替康（Irinotecan HCl）等前体药物；作为阳性对照品用于抗癌药物筛选。
临床研究：用于评估患者体内SN-38暴露量与疗效/毒副作用的相关性（药代动力学/药效学，PK/PD）。
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、多药耐药性（MDR）以及喜树碱类衍生物的构效关系（SAR）。

Pharmaceutical R&D: Used as a key intermediate for synthesizing or quality controlling prodrugs like Irinotecan Hydrochloride; serves as a positive control in anticancer drug screening.
Clinical Research: Used to evaluate the correlation between SN-38 exposure and efficacy/toxicity in patients (Pharmacokinetics/Pharmacodynamics, PK/PD).
Scientific Research: Acts as a Tool Compound to investigate the mechanism of Topo I inhibitors, tumor cell apoptosis pathways, multidrug resistance (MDR), and structure-activity relationships (SAR) of camptothecin 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, 10g）。
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, 10g).
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.