Irinotecan-d₅ hydrochloride  (Synonyms: 伊立替康盐酸盐-d₅; (+)-Irinotecan-d₅ hydrochloride; CPT-11-d₅ hydrochloride; VAL-413-d₅)

Irinotecan-d₅ hydrochloride is deuterated labeled Irinotecan hydrochloride (HY-16562A). Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer^[1].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
Irinotecan hydrochloride 是一种拓扑异构酶 I 抑制剂。Irinotecan hydrochloride 抑制 LoVo 和 HT-29 细胞的生长，IC₅₀ 分别为 15.8 ± 5.1 和 5.17 ± 1.4 μM，并在 LoVo 和 HT-29 中诱导相似数量的可裂解复合物细胞^[3]。Irinotecan hydrochloride 抑制人脐静脉内皮细胞 (HUVEC) 的增殖，IC₅₀ 为 1.3 μM^[4]。

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

Irinotecan hydrochloride (CPT-11 hydrochloride，5 mg/kg) 在大鼠体内连续两周每天瘤内注射显著抑制肿瘤的生长，这种作用也通过渗透性微型泵连续腹腔内输注到小鼠体内产生。然而，Irinotecan hydrochloride (10 mg/kg) 对腹腔内肿瘤的生长没有影响^[2]。
Irinotecan hydrochloride (CPT-11，100-300 mg/kg，ip) 在第 21 天明显抑制无胸腺雌性小鼠 HT-29 异种移植物的肿瘤生长。
Irinotecan hydrochloride (125 mg/kg) 加 TSP-1 (10 mg/kg 每天) 或 Irinotecan hydrochloride (150 mg/kg) 联合 TSP-1 (每天 20 mg/kg) 几乎同样有效，分别抑制肿瘤生长 84% 和 89%，联合使用都比单独使用 Irinotecan hydrochloride 更有效剂量为 250 和 300 mg/kg^[4]。

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

628.17

C₃₃H₃₄D₅ClN₄O₆

718612-73-8

100286-90-6

伊立替康盐酸盐-d₅

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. 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]

  [3]. 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]

  [4]. 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]