Irinotecan
(Synonyms: 伊立替康; (+)-Irinotecan; CPT-11) 目录号 : GC11473
Irinotecan是一种拓扑异构酶抑制剂，主要用于治疗结直肠癌。Irinotecan可通过与拓扑异构酶 I-DNA 复合物结合，阻止 DNA 链的再连接，并导致 DNA 双链断裂和细胞死亡 。
Cas No.:97682-44-5
Sample solution is provided at 25 µL, 10mM.
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| Cell experiment [1]: | |
Cell lines | LoVo and HT-29 cells |
Preparation Method | LoVo and HT-29 cells were exposed to different concentrations of irinotecan(0-80μg/ml; 24h ) to determine the IC50 values. |
Reaction Conditions | Irinotecan(0-80μg/ml; 24h ) |
Applications | The IC50 values of LoVo cells is 6μg/ml, and for HT-29 cells is 12μg/ml. |
| Animal experiment [2]: | |
Animal models | Ehrlich ascites tumour cells model |
Preparation Method | The mice were administered quercetin and naringin (100mg/kg ) daily for 3 consecutive days, beginning on day 3 after i.p. injection of Ehrlich ascites tumour cells. Irinotecan was administered i.p. at a dose of 50mg/kg on days 1, 13 and 19 . |
Dosage form | Irinotecan: 50mg/kg; ip; 1,13,19days |
Applications | Mice given a combination of irinotecan and flavonoids had a significantly decreased number of tumour cells in the peritoneal cavity as compared to non-treated mice but counts on macrophages, lymphocytes and neutrophils were significantly higher than in non-treated mice. |
References: | |
Irinotecan is a topoisomerase inhibitor used primarily for the treatment of colorectal cancer. Irinotecan binds to the topoisomerase I-DNA complex, preventing DNA strand reconnection and leading to DNA double-strand breaks and cell death[1].
Irinotecan(2μM; 48h) treatment with Panc-1 and MIA PaCa-2 resulted in 57.5% reduction of migratory in Panc-1 cells and in a 53.9% in MIA PaCa-2 cells [1]. In the cell cycle analysis, Irinotecan (0.3 to 30μM for 24-48h ) increased the proportions at the S and G2/M phases of cell cycling in parallel with a decreased population at the G1 phase in Caco-2 and CW2 cells [2].
For xenografted HCT116 cells, Irinotecan (10mg/kg; i.p; 5days) can reduced tumors by 80% and mice urvival was again improved (>16weeks vs 12weeks in mock ） without any mouse toxicity[3]. Irinotecan (20mg/kg/day; ip; days 1–3, 8–10) were treat with Prostatic small cell carcinoma (SCC) arrested xenograft growth with a small reduction in tumor volume and only minor weight loss of the hosts (7%)[4]. Mice given a combination of Irinotecan (50mg/kg; ip; 1,13,19days ) had a decreased number of tumour cells in the peritoneal cavity as compared to non-treated mice but counts on macrophages, lymphocytes and neutrophils were higher than in non-treated mice[5].
[1]. Rodriguez Lanzi C, Wei R, Luo D, Mackenzie GG. Phospho-Aspirin (MDC-22) inhibits pancreatic cancer growth in patient-derived tumor xenografts and KPC mice by targeting EGFR: Enhanced efficacy in combination with irinotecan. Neoplasia. 2022 Feb;24(2):133-144.
[2]. Kaku Y, Tsuchiya A, Kanno T, Nishizaki T. Irinotecan induces cell cycle arrest, but not apoptosis or necrosis, in Caco-2 and CW2 colorectal cancer cell lines. Pharmacology. 2015;95(3-4):154-9.
[3]. Sharma A, Vatapalli R, Abdelfatah E, Wyatt McMahon K, Kerner Z, A Guzzetta A, Singh J, Zahnow C, B Baylin S, Yerram S, Hu Y, Azad N, Ahuja N. Hypomethylating agents synergize with irinotecan to improve response to chemotherapy in colorectal cancer cells. PLoS One. 2017 Apr 26;12(4):e0176139.
[4]. Tung WL, Wang Y, Gout PW, Liu DM, Gleave M, Wang Y. Use of irinotecan for treatment of small cell carcinoma of the prostate. Prostate. 2011 May 15;71(7):675-81.
[5]. Sharma A, Vatapalli R, Abdelfatah E, Wyatt McMahon K, Kerner Z, A Guzzetta A, Singh J, Zahnow C, B Baylin S, Yerram S, Hu Y, Azad N, Ahuja N. Hypomethylating agents synergize with irinotecan to improve response to chemotherapy in colorectal cancer cells. PLoS One. 2017 Apr 26;12(4):e0176139.
Irinotecan是一种拓扑异构酶抑制剂，主要用于治疗结直肠癌。Irinotecan可通过与拓扑异构酶 I-DNA 复合物结合，阻止 DNA 链的再连接，并导致 DNA 双链断裂和细胞死亡 [1]。
Irinotecan（2μM；48h）处理 Panc-1 和 MIA PaCa-2 细胞后，Panc-1 细胞的迁移率降低了 57.5%，MIA PaCa-2 细胞的迁移率降低了 53.9%[1]。在细胞周期分析中，Irinotecan（0.3 至 30μM；24-48 h）增加了细胞周期 S 期和 G2/M 期的比例，同时减少了 Caco-2 和 CW2 细胞 G1 期的数量[2]。
对于异种移植的 HCT116 细胞的小鼠，Irinotecan（10mg/kg，po，5days）可使肿瘤缩小 80%，小鼠存活率提高（大于 16 周，模拟小鼠为 12 周），且无任何小鼠毒性[3]。Irinotecan（20mg/kg/day；ip；第 1-3 天和第 8-10 天）治疗前列腺小细胞癌（SCC）抑制了异种移植的生长，肿瘤体积略有缩小，宿主体重仅轻微下降（7%）[4]。与未接受治疗的小鼠相比，接受Irinotecan（50mg/kg；ip；1、13、19 天）治疗的小鼠腹腔中肿瘤细胞的数量减少，但巨噬细胞、淋巴细胞和中性粒细胞的数量明显高于未接受治疗的小鼠[5]。
| Cas No. | 97682-44-5 | SDF | |
| 别名 | 伊立替康; (+)-Irinotecan; CPT-11 | ||
| 化学名 | 4,11-diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl [1,4'-bipiperidine]-1'-carboxylate | ||
| Canonical SMILES | O=C(OC1)C(O)(CC)C2=C1C(N(CC3=C4N=C5C(C=C(OC(N6CCC(N7CCCCC7)CC6)=O)C=C5)=C3CC)C4=C2)=O | ||
| 分子式 | C33H38N4O6 | 分子量 | 586.68 |
| 溶解度 | >29.4mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7045 mL | 8.5225 mL | 17.0451 mL |
| 5 mM | 0.3409 mL | 1.7045 mL | 3.409 mL |
| 10 mM | 0.1705 mL | 0.8523 mL | 1.7045 mL |
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动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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