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Irinotecan

Catalog No. T6228 CAS 97682-44-5

Synonyms: CPT-11, Topotecin, (+)-Irinotecan

Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.

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Irinotecan, CAS 97682-44-5

Pack Size	Availability	Price/USD
10 mg	In stock	$ 29.00
25 mg	In stock	$ 40.00
50 mg	In stock	$ 58.00
100 mg	In stock	$ 88.00
200 mg	In stock	$ 127.00
500 mg	In stock	$ 229.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 100%

Purity: 99.92%

Purity: 99.9%

Purity: 99.31%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.
In vitro	METHODS: Human breast cancer cells MCF-7 were treated with Irinotecan (10-320 µg/mL) for 24-48 h. Cell viability was measured by trypan blue. RESULTS: Cell viability decreased to 85.5% at 10 µg/mL and 58% at 160 µg/mL with Irinotecan treatment for 24 h. Viability decreased to 33% at 160 µg/mL with Irinotecan treatment for 48 h. [1] METHODS: HCT116 p53+/+,hMLH1+, p53+/+,hMLH1- and p53-/-,hMLH1- were treated with Irinotecan (4.5 µM) for 48 h. Cell cycle profiles were analyzed by Flow Cytometry. RESULTS: Irinotecan treatment induced G2/M arrest of different durations in all three cell lines. The block was maintained for at least 12 days in the p53+/+, hMLH1+ cell lines. The slow release of the block in the p53+/+, hMLH1- cell line 6-9 days after treatment initiation suggests that the status of the hMLH1 molecule may indirectly or directly influence the maintenance of G2/M block. In the p53-/- cell line, G2/M block was terminated within 4 days of treatment initiation. [2]
In vivo	METHODS: To test the antitumor activity in vivo, Irinotecan (40 mg/kg) was administered intraperitoneally three times a week for four weeks to an NSG mouse model of MLL rearrangement ALL xenografts. RESULTS: Irinotecan effectively inhibited the growth of MLL rearrangement ALL in vivo. [3] METHODS: To assay anti-tumor activity in vivo, Irinotecan (10 mg/kg four times every four days or 40 mg/kg six times every four days) was administered intraperitoneally to swiss nu/nu mice bearing five CRC xenograft tumors. RESULTS: At low doses of Irinotecan, four of the five xenografts responded to Irinotecan with a growth delay of up to 10 days. At high doses of Irinotecan, five xenografts showed variable but significant responses. [4]
Cell Research	Irinotecan is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. To determine the effects of Irinotecan in combination with 5-FU, the MTT assay is used. Depending on the cell lines, 10,000 to 20,000 cells per well are seeded in 96-well plates and incubated for 24 h in complete medium. On day 2, cells are incubated in the absence or presence of Irinotecan for 30 min followed by 5-FU for 24 h. After another 24 h in complete medium without any additives, MTT reagent is added on day 4 to initiate the assay and the cells are incubated for an additional 4 h at 37°C. After removal of the medium and dissolving the crystals with acidified isopropanol, the samples are analyzed using an ELISA plate reader at 570 nm. The value at 650 nm is subtracted as background[1].
Source	Natural Products > Nyssaceae > Camptotheca

Synonyms	CPT-11, Topotecin, (+)-Irinotecan
Molecular Weight	586.68
Formula	C33H38N4O6
CAS No.	97682-44-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 32 mg/mL (54.5 mM), Sonication is recommended.

References and Literature

1. Keyvani-Ghamsari S, et al. Effect of irinotecan on HMGB1, MMP9 expression, cell cycle, and cell growth in breast cancer (MCF-7) cells. Tumour Biol. 2017 Apr;39(4):1010428317698354. 2. Magrini R, et al. Cellular effects of CPT-11 on colon carcinoma cells: dependence on p53 and hMLH1 status. Int J Cancer. 2002 Sep 1;101(1):23-31. 3. Kerstjens M, et al. Irinotecan Induces Disease Remission in Xenograft Mouse Models of Pediatric MLL-Rearranged Acute Lymphoblastic Leukemia. Biomedicines. 2021 Jun 23;9(7):711. 4. Bras-Gonçalves RA, et al. Sensitivity to CPT-11 of xenografted human colorectal cancers as a function of microsatellite instability and p53 status. Br J Cancer. 2000 Feb;82(4):913-23. 5. Zhu A, Ji Z, Zhao J, et al. Effect of Euphorbia factor L1 on intestinal barrier impairment and defecation dysfunction in Caenorhabditis elegans[J]. Phytomedicine. 2019: 153102.

Citations

1. Larson T S, Glish G L, Lockett M R. Spatially resolved quantification of drug metabolism and efficacy in 3D paper-based tumor mimics. Analytica Chimica Acta. 2021: 339091. 2. Zhu A, Ji Z, Zhao J, et al. Effect of Euphorbia factor L1 on intestinal barrier impairment and defecation dysfunction in Caenorhabditis elegans. Phytomedicine. 2019: 153102

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Traditional Chinese Medicine Monomer Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Pancreatic Cancer Compound Library Target-Focused Phenotypic Screening Library Pediatric Drug Library

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Keywords

Irinotecan 97682-44-5 Autophagy DNA Damage/DNA Repair Topoisomerase Inhibitor CPT-11 Topotecin CPT 11 CPT11 inhibit (+)-Irinotecan inhibitor

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