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盐酸依立替康三水合物 /Irinotecan HCl Trihydrate {[allProObj[0].p_purity_real_show]}

货号:A244220 同义名: 盐酸伊立替康三水合物 / CPT-11 hydrochloride trihydrate;Irinotecan (hydrochloride hydrate)

Irinotecan HCl Trihydrate是一种具有抗肿瘤活性的拓扑异构酶 I 抑制剂。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Irinotecan HCl Trihydrate 化学结构 CAS号:136572-09-3
Irinotecan HCl Trihydrate 化学结构
CAS号:136572-09-3
Irinotecan HCl Trihydrate 3D分子结构
CAS号:136572-09-3
Irinotecan HCl Trihydrate 化学结构 CAS号:136572-09-3
Irinotecan HCl Trihydrate 3D分子结构 CAS号:136572-09-3
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Irinotecan HCl Trihydrate 纯度/质量文件 产品仅供科研

货号:A244220 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 HCl Trihydrate 生物活性

靶点
  • Topo I

描述 Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate), a potent topoisomerase I inhibitor, exhibits antitumor properties[1].
体内研究

When administered as Irinotecan (CPT-11, 5 mg/kg) via intratumoral injection daily for five consecutive days over two weeks in rats, significant tumor growth inhibition is observed. This inhibitory effect is also noted with continuous intraperitoneal infusion using an osmotic minipump in mice. However, a dosage of 10 mg/kg by intraperitoneal injection does not affect tumor growth[1].

Additionally, Irinotecan (CPT-11, 100-300 mg/kg, i.p.) significantly diminishes the growth of HT-29 xenografts in athymic female mice by the 21st day. Combination therapies of Irinotecan (125 mg/kg) with TSP-1 (10 mg/kg per day) or Irinotecan (150 mg/kg) with TSP-1 (20 mg/kg per day) show nearly identical efficacy, reducing tumor growth by 84% and 89%, respectively. These combinations prove more effective than Irinotecan alone at doses of 250 and 300 mg/kg[3].

体外研究

Irinotecan effectively halts the growth of LoVo and HT-29 cells, achieving IC50 values of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively. In these cell lines, Irinotecan also prompts the formation of a comparable level of cleavable complexes[2].

Moreover, Irinotecan hinders the proliferation of human umbilical vein endothelial cells (HUVEC), evidenced by an IC50 of 1.3 μM[3].

Irinotecan HCl Trihydrate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00483834 Colorectal Cancer Phase 2 Completed - Canada, Ontario ... 展开 >> Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 收起 <<
NCT03245450 Refractory or Recurrent Solid ... 展开 >>Tumors Rhabdomyosarcoma Non-Rhabdomyosarcoma Soft Tissue Sarcoma Ewing Sarcoma 收起 << Phase 1 Phase 2 Recruiting June 30, 2021 Germany ... 展开 >> Uniklinik RWTH Aachen Kinderklinik Recruiting Aachen, Germany Charite Virchow Kinderklinik - CC17 Recruiting Berlin, Germany Uniklinik Essen AoR Kinderklinik Recruiting Essen, Germany Klinik fur Kinder und Jugendmed - KKJM Recruiting Frankfurt, Germany Uniklinik Freiburg Kindermedizin Klinik IV Recruiting Freiburg, Germany Uniklinik Gottingen Kindermedizin Recruiting Gottingen, Germany Kinderklinik Muenchen Schwabing Not yet recruiting Muenchen, Germany 收起 <<
NCT02015754 Colorectal Cancer Phase 2 Completed - United States, Maryland ... 展开 >> The Johns Hopkins Hospital Baltimore, Maryland, United States, 21287 收起 <<

Irinotecan HCl Trihydrate 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 HCl Trihydrate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.48mL

0.30mL

0.15mL

7.38mL

1.48mL

0.74mL

14.77mL

2.95mL

1.48mL

Irinotecan HCl Trihydrate 技术信息

CAS号136572-09-3
分子式C33H45ClN4O9
分子量 677.185
别名 盐酸伊立替康三水合物 ;CPT-11 hydrochloride trihydrate;Irinotecan (hydrochloride hydrate);CPT-11 HCl Trihydrate;Irinotecan HCl Trihydrate;(+)-Irinotecan hydrochloride trihydrate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 50 mg/mL(73.84 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

H2O: 1.5 mg/mL(2.22 mM)

无水乙醇: 3 mg/mL(4.43 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方

IP 2% DMSO+water 8 mg/mL clear

PO 0.5% CMC-Na 48 mg/mL suspension

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