| CAS |
97682-44-5 |
| Chinese Name |
伊立替康 |
| English Name |
Irinotecan |
| Synonyms |
(+)-Irinotecan;Topotecin;CPT-11 |
| Molecular Formula |
C33H38N4O6 |
| Molecular Weight |
586.68 |
| Solubility |
Soluble in DMSO ≥10mg/mL |
| Purity |
HPLC≥98% |
| Appearance |
Light yellow to yellow Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 691-567-9 |
| MDL |
MFCD01862255 |
| SMILES |
O=C(N1CCC(N2CCCCC2)CC1)OC3=CC=C4N=C5C(CN6C(C(COC([C@@]7(CC)O)=O)=C7C=C65)=O)=C(CC)C4=C3 |
| InChIKey |
UWKQSNNFCGGAFS-XIFFEERXSA-N |
| InChI |
InChI=1S/C33H38N4O6/c1-3-22-23-16-21(43-32(40)36-14-10-20(11-15-36)35-12-6-5-7-13-35)8-9-27(23)34-29-24(22)18-37-28(29)17-26-25(30(37)38)19-42-31(39)33(26,41)4-2/h8-9,16-17,20,41H,3-7,10-15,18-19H2,1-2H3/t33-/m0/s1 |
| PubChem CID |
60838 |
| Target Point |
Topoisomerase |
| Passage |
DNA Damage/DNA Repair |
| Background |
Irinotecan is a topoisomerase I inhibitor that prevents religation of DNA strands by binding to the topoisomerase I-DNA complex. |
| Biological Activity |
Irinotecan是水溶性的拓扑异构酶I抑制剂，通过与拓扑异构酶I-DNA复合物结合来防止DNA链的再连接。[1-5] |
| In Vitro |
伊立替康是拓扑异构酶I抑制剂。伊立替康抑制LoVo和HT-29细胞的生长，IC50分别为15.8±5.1和5.17±1.4μM，并且在LoVo和HT-29细胞中诱导相似量的可切割复合物[2]。伊立替康抑制人脐静脉内皮细胞(HUVEC)的增殖，IC50为1.3μM[3]。 |
| In Vivo |
伊立替康(CPT-11，5mg / kg)在大鼠中连续两周每天通过肿瘤内注射显着抑制肿瘤的生长，并且这种效果也通过渗透微型泵连续腹膜内输注进入小鼠而发生。然而，伊立替康(10 mg / kg)对ip的生长没有影响[1]。伊立替康(CPT-11，100-300mg / kg，ip)显然在第21天抑制无胸腺雌性小鼠中HT-29异种移植物的肿瘤生长。两组伊立替康(125mg / kg)加TSP-1(10mg)/ kg /天或伊立替康(150 mg / kg)联合使用TSP-1(每天20 mg / kg)几乎同样有效，分别抑制肿瘤生长84％和89％，两者均比单独使用伊立替康更有效剂量为250和300毫克/千克[3]。 |
| Cell Experiment |
将指数生长的细胞接种在20cm 2培养皿中，每个细胞系具有最佳细胞数(对于LoVo细胞为20，000，对于HT-29细胞为100，000)。 2天后，用增加浓度的伊立替康或SN-38处理它们一个细胞倍增时间(LoVo细胞24小时，HT-29细胞40小时)。用0.15M NaCl洗涤后，细胞在正常培养基中进一步生长两次，用胰蛋白酶-EDTA从支持物上分离，并在血细胞计数器中计数。然后将IC50值估计为与不用药物孵育的细胞相比，负责50％生长抑制的药物浓度[2]。 |
| Animal Experiment |
伊立替康通过瘤内注射0.1cc体积的适当溶液给药，连续两周每天5mg / kg，连续两周，然后休息7天，称为一个治疗周期。大鼠在8周的时间内接受三个周期。对照动物通过瘤内注射以与第II组动物相同的给药规则接受0.1cc无菌0.9％氯化钠溶液[1]。 |
| Data Literature Source |
[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.
[4]. Dela Cruz FS， et al. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. Genome Med. 2016 Oct 31; 8 (1) :116.
[5]. Huang MY， et al. Chemotherapeutic agent CPT-11 eliminates peritoneal resident macrophages by inducing apoptosis. Apoptosis. 2016 Feb; 21 (2) :130-42. |
| Unit |
Bottle |
| Specification |
10mg 10mM*1mL in DMSO 50mg |
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