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Irinotecan

Catalog No.GC11473

Irinotecan is a topoisomerase inhibitor used primarily for the treatment of colorectal cancer. Irinotecan binds to the topoisomerase I-DNA complex, preventing DNA strand reconnection and leading to DNA double-strand breaks and cell death.

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Irinotecan Chemical Structure

Cas No.: 97682-44-5

Size Price Stock Qty
10mM (in 1mL DMSO)
$40.00
In stock
100mg
$36.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Description of Irinotecan

Irinotecan is a topoisomerase inhibitor used primarily for the treatment of colorectal cancer. Irinotecan binds to the topoisomerase I-DNA complex, preventing DNA strand reconnection and leading to DNA double-strand breaks and cell death[1].

Irinotecan(2μM; 48h) treatment with Panc-1 and MIA PaCa-2 resulted in 57.5% reduction of migratory in Panc-1 cells and in a 53.9% in MIA PaCa-2 cells [1]. In the cell cycle analysis, Irinotecan (0.3 to 30μM for 24-48h ) increased the proportions at the S and G2/M phases of cell cycling in parallel with a decreased population at the G1 phase in Caco-2 and CW2 cells [2].

For xenografted HCT116 cells, Irinotecan (10mg/kg; i.p; 5days) can reduced tumors by 80% and mice urvival was again improved (>16weeks vs 12weeks in mock ) without any mouse toxicity[3]. Irinotecan (20mg/kg/day; ip; days 1–3, 8–10) were treat with Prostatic small cell carcinoma (SCC) arrested xenograft growth with a small reduction in tumor volume and only minor weight loss of the hosts (7%)[4]. Mice given a combination of Irinotecan (50mg/kg; ip; 1,13,19days ) had a decreased number of tumour cells in the peritoneal cavity as compared to non-treated mice but counts on macrophages, lymphocytes and neutrophils were higher than in non-treated mice[5].

[1]. Rodriguez Lanzi C, Wei R, Luo D, Mackenzie GG. Phospho-Aspirin (MDC-22) inhibits pancreatic cancer growth in patient-derived tumor xenografts and KPC mice by targeting EGFR: Enhanced efficacy in combination with irinotecan. Neoplasia. 2022 Feb;24(2):133-144.
[2]. Kaku Y, Tsuchiya A, Kanno T, Nishizaki T. Irinotecan induces cell cycle arrest, but not apoptosis or necrosis, in Caco-2 and CW2 colorectal cancer cell lines. Pharmacology. 2015;95(3-4):154-9.
[3]. Sharma A, Vatapalli R, Abdelfatah E, Wyatt McMahon K, Kerner Z, A Guzzetta A, Singh J, Zahnow C, B Baylin S, Yerram S, Hu Y, Azad N, Ahuja N. Hypomethylating agents synergize with irinotecan to improve response to chemotherapy in colorectal cancer cells. PLoS One. 2017 Apr 26;12(4):e0176139.
[4]. Tung WL, Wang Y, Gout PW, Liu DM, Gleave M, Wang Y. Use of irinotecan for treatment of small cell carcinoma of the prostate. Prostate. 2011 May 15;71(7):675-81.
[5]. Sharma A, Vatapalli R, Abdelfatah E, Wyatt McMahon K, Kerner Z, A Guzzetta A, Singh J, Zahnow C, B Baylin S, Yerram S, Hu Y, Azad N, Ahuja N. Hypomethylating agents synergize with irinotecan to improve response to chemotherapy in colorectal cancer cells. PLoS One. 2017 Apr 26;12(4):e0176139.

Protocol of Irinotecan

Cell experiment [1]:

Cell lines

LoVo and HT-29 cells

Preparation Method

LoVo and HT-29 cells were exposed to different concentrations of irinotecan(0-80μg/ml; 24h ) to determine the IC50 values.

Reaction Conditions

Irinotecan(0-80μg/ml; 24h )

Applications

The IC50 values of LoVo cells is 6μg/ml, and for HT-29 cells is 12μg/ml.
Animal experiment [2]:

Animal models

Ehrlich ascites tumour cells model

Preparation Method

The mice were administered quercetin and naringin (100mg/kg ) daily for 3 consecutive days, beginning on day 3 after i.p. injection of Ehrlich ascites tumour cells. Irinotecan was administered i.p. at a dose of 50mg/kg on days 1, 13 and 19 .

Dosage form

Irinotecan: 50mg/kg; ip; 1,13,19days 

Applications

Mice given a combination of irinotecan and flavonoids had a significantly decreased number of tumour cells in the peritoneal cavity as compared to non-treated mice but counts on macrophages, lymphocytes and neutrophils were significantly higher than in non-treated mice.

References:
[1]. Huang YF, Zhu DJ, Chen XW, Chen QK, Luo ZT, Liu CC, Wang GX, Zhang WJ, Liao NZ. Curcumin enhances the effects of irinotecan on colorectal cancer cells through the generation of reactive oxygen species and activation of the endoplasmic reticulum stress pathway. Oncotarget. 2017 Jun 20;8(25):40264-40275.
[2]. Knežević AH, Dikić D, Lisičić D, Kopjar N, Oršolić N, Karabeg S, Benković V. Synergistic effects of irinotecan and flavonoids on Ehrlich ascites tumour-bearing mice. Basic Clin Pharmacol Toxicol. 2011 Nov;109(5):343-9.

Chemical Properties of Irinotecan

Cas No. 97682-44-5 SDF
Chemical Name 4,11-diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl [1,4'-bipiperidine]-1'-carboxylate
Canonical SMILES O=C(OC1)C(O)(CC)C2=C1C(N(CC3=C4N=C5C(C=C(OC(N6CCC(N7CCCCC7)CC6)=O)C=C5)=C3CC)C4=C2)=O
Formula C33H38N4O6 M.Wt 586.68
Solubility >29.4mg/mL in DMSO Storage 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Irinotecan

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1 mg 5 mg 10 mg
1 mM 1.7045 mL 8.5225 mL 17.0451 mL
5 mM 340.9 μL 1.7045 mL 3.409 mL
10 mM 170.5 μL 852.3 μL 1.7045 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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