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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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+ |
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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。 |
靶点 |
|
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]. |
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 << |
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 |
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 |