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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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有货
概述
Irinotecan是一种Topoisomerase I抑制剂，作用于LoVo细胞和HT-29细胞，IC50分别为15.8 μM和5.17 μM。
Information
Irinotecan (CPT-11, (+)-Irinotecan) is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.
In vitro
Irinotecan is activated to SN-38 by carboxylesterases to become able to interact with its target, topoisomerase I. Irinotecan induces similar amounts of cleavable complexes at its IC50 in LoVo cells and HT-29 cell lines. SN-38 induces a concentration-dependent formation of cleavable complexes, which is not significantly different in LoVo cells and HT-29 cell lines. Cell accumulation of Irinotecan is markedly different, reaching consistently higher levels in HT-29 cells than in LoVo cells. The lactone E-ring of Irinotecan and SN-38 hydrolyses reversibly in aqueous solutions, and the interconversion between the lactone and carboxylate forms is dependent on pH and temperature. Liver is primarily responsible for the activation of Irinotecan to SN-38. At equal concentrations of Irinotecan and SN-38 glucuronide, the rate of beta-glucuronidase-mediated SN-38 production is higher than that formed from Irinotecan in both tumour and normal tissue. Irinotecan is also converted to SN-38 in intestines, plasma and tumor tissues. Irinotecan is significantly more active in SCLC than in NSCLC cell lines, whereas no significant difference between histological types is observed with SN-38.
In vivo
In COLO 320 xenografts, Irinotecan induces a maximum growth inhibition of 92%. A single dose of Irinotecan significantly increases amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver. Concomitantly, the Irinotecan-treated group shows significantly higher amounts of DNA strand breaks in colon mucosa cells compared to the control group.
Cell Data
cell lines：
Concentrations：0 μM -100 μM
Incubation Time：48 hours
Powder Purity:≥99%
规格
别名
伊立替康（CPT-11）
英文别名
(+)-Irinotecan
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Irinotecan (CPT-11)
生化机理
伊立替康（CPT-11，(+)-伊立替康）是一种拓扑异构酶 I 抑制剂，对 LoVo 细胞和 HT-29 细胞的 IC50 分别为 15.8 μM 和 5.17 μM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
DNA 拓扑异构酶 I 抑制剂
名称和识别符
EC号
691-567-9
分子类型
小分子
Isomeric SMILES
CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)[C@@]4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7
分子量
586.68
Reaxy-Rn
4285693
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4285693&ln=
高级数据
关联靶点（人）
ACHE
Tclin
乙酰胆碱酯酶(Acetylcholinesterase)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 71 mg/mL (200.89 mM); Ethanol: 71 mg/mL (200.89 mM); Water: Insoluble;
安全和危险性（GHS）
信号词
危险
危险声明
H302: 吞食有害
H315: 引起皮肤刺激
H318: 造成严重的眼睛损伤
H361: 怀疑破坏生育力或未出生的孩子
H373: 长期或反复接触可能对器官造成伤害
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
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