Irinotecan  (Synonyms: 伊立替康; (+)-Irinotecan; CPT-11; VAL-413(free base))

Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex^[1].

Irinotecan 是一种拓扑异构酶 I 抑制剂。Irinotecan 抑制 LoVo 和 HT-29 细胞的生长，IC₅₀ 分别为 15.8 和 5.17 μM，并在 LoVo 和 HT-29 细胞中诱导相似量的可裂解复合物^[2]。
Irinotecan 抑制人脐静脉内皮细胞 (HUVEC) 的增殖，IC₅₀ 为 1.3 μM^[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Irinotecan（CPT-11，5 mg/kg）连续5天每天瘤内注射，连续2周，可显著抑制大鼠肿瘤生长，通过渗透微泵持续腹膜内输注给小鼠也能看到这种效果。然而，Irinotecan（10 mg/kg）腹腔注射对肿瘤生长没有影响^[1]。
Irinotecan (CPT-11, 100-300 mg/kg, ip) 在第 21 天明显抑制了无胸腺雌性小鼠中 HT-29 异种移植瘤的肿瘤生长。Irinotecan (125 mg/kg) 加 TSP-1 (10 mg/kg/天) 或 Irinotecan (150 mg/kg) 加 TSP-1 (20 mg/kg/天) 两组疗效几乎相同，分别抑制肿瘤生长 84% 和 89%，且均比单独使用 Irinotecan (250 和 300 mg/kg 剂量) 更有效^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

586.68

C₃₃H₃₈N₄O₆

97682-44-5

固体

White to yellow

伊立替康；依立替康

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* 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, 6 months; -20°C, 1 month (protect from light)。-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。

• [1]. Morales C, et al. Antitumoral effect of irinotecan (CPT-11) on an experimental model of malignant neuroectodermal tumor. J Neurooncol. 2002 Feb;56(3):219-26.  [Content Brief]

  [2]. Pavillard V, et al. Determinants of the cytotoxicity of irinotecan in two human colorectal tumor cell lines. Cancer Chemother Pharmacol. 2002 Apr;49(4):329-35. Epub 2002 Jan 30.  [Content Brief]

  [3]. Allegrini G, et al. Thrombospondin-1 plus irinotecan: a novel antiangiogenic-chemotherapeutic combination that inhibits the growth of advanced human colon tumor xenografts in mice. Cancer Chemother Pharmacol. 2004 Mar;53(3):261-6. Epub 2003 Dec 5.  [Content Brief]

  [4]. Dela Cruz FS, et al. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. Genome Med. 2016 Oct 31;8(1):116.  [Content Brief]

  [5]. Huang MY, et al. Chemotherapeutic agent CPT-11 eliminates peritoneal resident macrophages by inducing apoptosis. Apoptosis. 2016 Feb;21(2):130-42.  [Content Brief]