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Irinotecan

Irinotecan is an analog of camptothecin that is used clinically to treat colon and ovarian cancers, among others. Irinotecan exhibits anticancer chemotherapeutic, anti-angiogenic, and immunosuppressive activities. Irinotecan inhibits DNA topoisomerase I and sensitizes tumors to the effects of radiation. In glioma models, irinotecan decreases the number of tumor vessels and decreases expression of VEGF and HIF-1α, inhibiting tumor growth. Irinotecan also moderates inhibition of dendritic cell differentiation and may produce cholinergic side effects, suggesting potential inhibition of acetylcholinesterase (AChE) as well.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18931708

Cas No.

97682-44-5

Purity

≥98%

Formula

C33H38N4O6

Formula Wt.

586.68

Chemical Name

[1,4-Bipiperidine]-1-carboxylic acid (4S)-4,11- diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo- 1H-pyrano[3,4:6,7]indolizino[1,2-b]quinolin-9-yl ester

Solubility

Insoluble in water. Soluble in DMSO

Appearance

Pale Yellow Powder

Hu J, Kinn J, Zirakzadeh AA, et al. The effects of chemotherapeutic drugs on human monocyte-derived dendritic cell differentiation and antigen presentation. Clin Exp Immunol. 2013 Jun;172(3):490-9. PMID: 23600838.

Pan P, Li Y, Yu H, et al. Molecular principle of topotecan resistance by topoisomerase I mutations through molecular modeling approaches. J Chem Inf Model. 2013 Apr 22;53(4):997-1006. PMID: 23521602.

Chen AY, Chen PM, Chen YJ. DNA topoisomerase I drugs and radiotherapy for lung cancer. J Thorac Dis. 2012 Aug;4(4):390-7. PMID: 22934142.

Chintala S, Tóth K, Cao S, et al. Se-methylselenocysteine sensitizes hypoxic tumor cells to irinotecan by targeting hypoxia-inducible factor 1alpha. Cancer Chemother Pharmacol. 2010 Oct;66(5):899-911. PMID: 20066420.

Dodds HM, Rivory LP. The mechanism for the inhibition of acetylcholinesterases by irinotecan (CPT-11). Mol Pharmacol. 1999 Dec;56(6):1346-53. PMID: 10570064.

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