Home > Topoisomerase & > Irinotecan HCl Trihydrate

Irinotecan HCl Trihydrate

盐酸伊立替康三水合物,CPT-11 HCl Trihydrate

Irinotecan HCl Trihydrate通过抑制Topoisomerase 1（拓扑异构酶1）而防止DNA解链。

目录号
EY0863
EY0863
纯度
99.39%
99.39%
规格
50 mg
100 mg
原价
580
960
售价
580
960
库存
现货
现货
订购
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  • 生物活性

    Irinotecan hydrochloride trihydrate, a compound within the camptothecin family, is an inhibitor of Topo I (topoisomerase I) involved in cellular DNA replication and transcription. Irinotecan HCl Trihydrate is hydrochloride form of Irinotecan. Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. As a Topo I inhibitor, Irinotecan inhibits the religation step of the enzyme's normal action, inducing single stranded DNA breaks. These single stranded breaks are then converted to double-stranded breaks within the course of DNA replication which is reported to induce apoptosis or repair mechanisms as a result.

  • 体外研究

  • 体内研究

    30% propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)

  • 激酶实验

  • 细胞实验

    0 μM -100 μM

  • 动物实验

    20 mg/kg 腹腔注射

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Pavillard V, et al. Cancer Chemother Pharmacol. 2002, 49(4), 329-335.
    [2] Worden, F.P. et al. 2000. Expert Opin Investig Drugs. 9: 565-579.
    [3] Kellner, U., et al. 2000. Onkologie. 23: 424-430.
    [4] Takeba, Y., et al. 2007. J. Pharmacol. Sci. 104: 232-242.

    分子式
    C33H38N4O6.HCl.3H2O    		 分子量
    677.18    		 CAS号
    136572-09-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    1 mg/mL    		 Ethanol
    >5 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00003225 Colorectal Cancer Drug: amifostine trihydrate|Drug: irinotecan hydrochloride Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI)|ALZA Phase 1|Phase 2 1997-07-01 2015-09-30
    NCT00160875 Esophageal Cancer Drug: Irinotecan hydrochloride trihydrate|Drug: Cisplatin University Health Network, Toronto|Pfizer Phase 2|Phase 3 2009-04-01 2016-07-29
    NCT00693719 Breast Cancer Drug: Etoposide|Drug: Irinotecan hydrochloride University of Arizona|National Cancer Institute (NCI) Phase 2 2007-08-01 2015-10-15
    NCT00393094 High-Grade Gliomas Biological: Bevacizumab|Drug: Irinotecan hydrochloride National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 2 2006-09-01 2012-07-06
    NCT00004919 Unspecified Childhood Solid Tumor, Protocol Specific Drug: cisplatin|Drug: irinotecan hydrochloride|Drug: amifostine trihydrate|Other: pharmacological study National Cancer Institute (NCI) Phase 1 1999-12-01 2013-07-01
    NCT00483834 Colorectal Cancer Drug: Bevacizumab|Drug: Irinotecan|Drug: Capecitabine University Health Network, Toronto|Hoffmann-La Roche Phase 2 2006-12-01 2012-03-19
    NCT02015754 Colorectal Cancer Drug: DEBIRI|Device: LC Bead M1|Procedure: TACE Yale University Phase 2 2014-02-01 2017-03-08
    NCT01494506 Metastatic Pancreatic Cancer Drug: MM-398|Drug: 5 Fluorouracil|Drug: Leucovorin Merrimack Pharmaceuticals Phase 3 2011-11-01 2016-06-16

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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