| Bioactivity | 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]. |
| Invitro | 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. 0 --> Irinotecan-d5 hydrochloride 相关抗体: |
| In Vivo | 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. |
| CAS | 718612-73-8 |
| Formula | C33H34D5ClN4O6 |
| Molar Mass | 628.17 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [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. [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. [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. |
Irinotecan-d5 hydrochloride
CAS: 718612-73-8 F: C33H34D5ClN4O6 W: 628.17
Irinotecan-d5 hydrochloride is deuterated labeled Irinotecan hydrochloride (HY-16562A). Irinotecan hydrochloride ((+)-Ir
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This product is for research use only, not for human use. We do not sell to patients.