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伊立替康 /Irinotecan {[allProObj[0].p_purity_real_show]}

货号:A164809 同义名: CPT-11;VAL-413(free base)

Irinotecan是一种拓扑异构酶 I (topoisomerase I) 抑制剂,可用于结肠癌和直肠癌的研究。

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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Irinotecan 化学结构 CAS号:97682-44-5
Irinotecan 化学结构
CAS号:97682-44-5
Irinotecan 3D分子结构
CAS号:97682-44-5
Irinotecan 化学结构 CAS号:97682-44-5
Irinotecan 3D分子结构 CAS号:97682-44-5
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Irinotecan 纯度/质量文件 产品仅供科研

货号:A164809 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Topo I Topo II Topo IV Topoisomerase 其他靶点 纯度
Ellagic acid 98%
β-Lapachone 99%+
(s)-10-hydroxycamptothecin 98+%
Camptothecin ++

Topo I, IC50: 0.68 μM

98%
Betulinic acid ++

Eukaryotic topoisomerase I, IC50: 5 μM

98%
Topotecan ++++

Topo I (MCF-7 Luc cells), IC50: 13 nM

Topo I (DU-145 Luc cells), IC50: 2 nM

98%
Irinotecan HCl Trihydrate 98%
SN-38 98%
Levofloxacin hydrate 98%
Dexrazoxane 99%+
Ofloxacin 98+%
Enoxacin 99%+
Flumequine +

Topo II, IC50: 15 μM

98%
Levofloxacin 97%
Etoposide 98%
Pefloxacin mesylate dihydrate 99+%
Marbofloxacin 98+%
Voreloxin HCl 98%
Mitoxantrone dihydrochloride PKC 98%
Nalidixic acid 98%
Doxorubicin 98%
Novobiocin sodium 95%
Amonafide 99%+
Pirarubicin 98%+
Idarubicin HCl +++

Topo II (MCF-7 cells), IC50: 3.3 ng/mL

99%+
Genistein EGFR 98%
Teniposide 98%
Moxifloxacin 98%
Ciprofloxacin 98%
Clinafloxacin 97%
Gatifloxacin 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Epirubicin HCl 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Irinotecan 生物活性

描述 Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor by preventing the DNA strand's religation through its binding to the topoisomerase I-DNA complex[1].
体内研究

Administered as Irinotecan (CPT-11, 5 mg/kg) through daily intratumoral injections for five days across two successive weeks in rats, and via continuous intraperitoneal infusion using an osmotic minipump in mice, it notably impedes tumor growth, whereas a dosage of 10 mg/kg exhibits no significant tumor growth inhibition by intraperitoneal injection[1].

Furthermore, Irinotecan (CPT-11, 100-300 mg/kg, i.p.) markedly diminishes tumor growth in HT-29 xenografts within athymic female mice by the 21st day. Combination treatments of Irinotecan (125 mg/kg) with TSP-1 (10 mg/kg per day) and Irinotecan (150 mg/kg) with TSP-1 (20 mg/kg per day) achieve tumor growth inhibition rates of 84% and 89%, respectively, surpassing the efficacy of Irinotecan alone at dosages of 250 and 300 mg/kg[3].

体外研究

As a potent topoisomerase I inhibitor, Irinotecan curtails the proliferation of LoVo and HT-29 cells, presenting IC50 values of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively, and similarly induces cleavable complexes in both cell types[2].

Irinotecan also hampers the growth of human umbilical vein endothelial cells (HUVEC), showcasing an IC50 of 1.3 μM[3].

Irinotecan 动物研究

Dose Mice: 5 mg/kg - 75 mg/kg[3] (p.o./i.v.) MTD: 240 mg/kg[4] (i.p., BALB/c Mice) Rat: 65 mg/kg - 130 mg/kg[5] (i.v.)
Administration p.o., i.v., i.p.
Pharmacokinetics
Animal Mice[3]
Dose 10 mg/kg
Administration i.v. or p.o.
Tmax 1 h (p.o.)
T1/2β 2.1 h (i.v.)
1.1 h (p.o.)
CL 24.8 L/h/m2 (i.v.)
Cmax 1796 ng/ml (i.v.)
74 ng/ml (p.o.)
AUC0→∞ 1301 ng·h/ml (i.v.)
154 ng·h/ml (p.o.)
Vss 21.6 L/kg (i.v.)

Irinotecan 参考文献

[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.

[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.

[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.

Irinotecan 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.52mL

1.70mL

0.85mL

17.05mL

3.41mL

1.70mL

Irinotecan 技术信息

CAS号97682-44-5
分子式C33H38N4O6
分子量 586.678
别名 CPT-11;VAL-413(free base);(+)-Irinotecan
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 25 mg/mL(42.61 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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