产品名称

盐酸伊立替康

Irinotecan Hydrochloride

化学名称

(4S)-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-基-[1,4'-联哌啶]-1'-甲酸酯盐酸盐三水合物

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

核心类别

喜树碱（Camptothecin）半合成衍生物，拓扑异构酶I（Topo I）抑制剂。

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

植物来源

最初来源于喜树 (Camptotheca acuminataDecne.)，本产品为半合成制得。

Originally derived from Camptotheca acuminata Decne., this product is semisynthetically prepared.

外观性状

淡黄色至黄色的疏松块状物或粉末，无臭。

Pale yellow to yellow loose masses or powder, odorless.

主要规格

医药级 (Pharma Grade)：
- 含量 (Assay): ≥99.0% (HPLC)
- 单一杂质: ≤0.5% (HPLC)
- 水分: 8.0% ~ 10.0% (Karl Fischer)
- 细菌内毒素: <0.5 EU/mg
科研级 (Research Grade)：
- 纯度: ≥99.5% (HPLC)
- 内毒素: <0.05 EU/mg

Pharmaceutical Grade:
- Assay: ≥99.0% (HPLC)
- Single Impurity: ≤0.5% (HPLC)
- Water Content: 8.0% ~ 10.0% (Karl Fischer)
- Bacterial Endotoxins: <0.5 EU/mg
Research Grade:
- Purity: ≥99.5% (HPLC)
- Endotoxins: <0.05 EU/mg

检测方法

HPLC, Titration, Karl Fischer

HPLC, Titration, Karl Fischer

CAS No.

100286-90-6 (无水物: 115385-88-9)

100286-90-6 (Anhydrous: 115385-88-9)

分子式

C₃₃H₃₈N₄O₆·HCl·3H₂O

C₃₃H₃₈N₄O₆·HCl·3H₂O

分子量

677.19 (无水物: 623.14)

677.19 (Anhydrous: 623.14)

药理功效

1. 强效抗肿瘤 (Potent Antitumor)：核心功效。作为前体药物，在体内经羧酸酯酶转化为活性代谢产物SN-38，特异性抑制拓扑异构酶I（Topo I），阻断DNA复制和转录，诱导肿瘤细胞凋亡。
2. 广谱抗癌 (Broad-spectrum Anticancer)：对结直肠癌（一线用药）、小细胞肺癌、胰腺癌、胃癌、卵巢癌等均有显著疗效。
3. 细胞周期特异性 (Cell Cycle Specificity)：主要作用于S期（DNA合成期）细胞。

1. Potent Antitumor: Core function. As a prodrug, it is converted in vivo by carboxylesterases to the active metabolite SN-38, which specifically inhibits Topoisomerase I (Topo I), blocking DNA replication and transcription, thereby inducing tumor cell apoptosis.
2. Broad-spectrum Anticancer: Effective against colorectal cancer (first-line treatment), small cell lung cancer, pancreatic cancer, gastric cancer, ovarian cancer, etc.
3. Cell Cycle Specificity: Primarily acts on cells in the S phase (DNA synthesis phase).

应用领域

医药制造：作为原料药 (API)，用于生产盐酸伊立替康注射剂（如市售品牌“开普拓”/Campto的仿制药）。
临床研究：作为化疗药物，用于癌症临床试验（I期、II期、III期）的研究。
科研：作为Topo I抑制剂的标准品，用于抗癌药物筛选、作用机制研究、耐药性研究。

Pharmaceutical Manufacturing: Used as an API (Active Pharmaceutical Ingredient) for producing Irinotecan Hydrochloride Injections (e.g., generics of the brand "Campto").
Clinical Research: Used as a chemotherapeutic agent in clinical trials (Phase I, II, III) for cancer.
Scientific Research: Used as a reference standard for Topo I inhibitors in anticancer drug screening, mechanism of action studies, and drug resistance research.

包装储存

关键提示：本品为细胞毒性药物，操作时需穿戴防护装备，并在指定区域操作。
包装：双层无菌聚乙烯袋封装，外加铝听或纸板桶（1kg, 5kg, 10kg/桶）。
储存：密封，避光，在2-8°C（冷藏）条件下保存，严防冻结。远离儿童。

Critical Note: This product is a cytotoxic drug. Wear protective equipment and operate in designated areas.
Packaging: Double-layer sterile polyethylene bag sealing, packed in aluminum cans or cardboard drums (1kg, 5kg, 10kg/drum).
Storage: Sealed, protected from light, store at 2-8°C (refrigerated), protect from freezing. Keep out of reach of children.