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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
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].
Irinotecan HCl Trihydrate/盐酸依立替康三水合物 细胞实验
Cell Line
Concentration
Treated Time
Description
References
pig fetal fibroblasts (PFFs)
1-10 µM
48 h
Dose-dependent increase in knock-in (KI) efficiency
Cell Biosci. 2023 Nov 25;13(1):215.
SK72 cells
30 μM
Irinotecan showed anti-GBM activity in SK72 cells with an IC50 value of 30 μM.
J Transl Med. 2014 Jan 17;12:13.
HT-29
20 µM
1.5 h
To investigate the effects of irinotecan alone or in combination with 5-FU on the growth, metabolic activity, proliferation, and clonogenic survival of HT-29 cells. Results showed that irinotecan alone or in combination with 5-FU significantly inhibited the growth, metabolic activity, and clonogenic survival of HT-29 cells, and significantly increased the radiosensitivity of tumor cells.
Int J Mol Sci. 2023 Jun 20;24(12):10385.
EC-109
0–125 μM
48 h
To evaluate the inhibitory effect of Irinotecan on the proliferation of EC-109 cells, the results showed that Irinotecan significantly inhibited cell proliferation at micromolar concentrations.
Cell Death Dis. 2018 May 31;9(6):661.
KYSE-450
0–125 μM
48 h
To evaluate the inhibitory effect of Irinotecan on the proliferation of KYSE-450 cells, the results showed that Irinotecan significantly inhibited cell proliferation at micromolar concentrations.
Cell Death Dis. 2018 May 31;9(6):661.
293T cells
10 µM
24 h
Increased the proportion of cells in S and G2/M phases, promoting CRISPR/Cas9-mediated homology-directed repair (HDR) efficiency
Cell Biosci. 2023 Nov 25;13(1):215.
BHK-21 cells
1-10 µM
48 h
Dose-dependent increase in dsDNA and ssODN-mediated knock-in (KI) efficiency
Cell Biosci. 2023 Nov 25;13(1):215.
SW480 cells
10 μM
48 h
To evaluate the effect of Irinotecan on SW480 cells, results showed decreased cell viability after Irinotecan treatment.
J Exp Clin Cancer Res. 2020 Jan 8;39(1):2.
U87 cells
10 μM
72 h
Irinotecan showed anti-GBM activity in U87 cells with an IC50 value lower than other compounds.
J Transl Med. 2014 Jan 17;12:13.
Irinotecan HCl Trihydrate/盐酸依立替康三水合物 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
C57BL/6J mice
Intraperitoneal injection
24 mg/kg
3 times per week for 9 weeks
To evaluate the effect of FOLFIRI on, lean mass, and fat mass in mice. FOLFIRI significantly reduced, lean mass, and fat mass, and increased the expression of markers of cellular senescence.
JCI Insight. 2024 Jan 23;9(2):e169512.
Mice
C57BL/6 mice
Intravenous injection
40 mg/kg
Every 3 or 4 days for 4 to 6 administrations
In the orthotopic MC38 tumor model, the Ir-silicasome demonstrated improved pharmacokinetics and tumor drug content compared to free drug and Onivyde?, significantly enhancing therapeutic efficacy, prolonging survival, and reducing bone marrow and gastrointestinal toxicity.
ACS Nano. 2019 Jan 22;13(1):38-53
BALB/c nude mice
Subcutaneous xenograft model
Intraperitoneal injection
5 mg/kg
Twice per week, for approximately 50 days
To study the role of eIF3a in irinotecan sensitivity in vivo, it was found that eIF3a silencing significantly increased tumor resistance to irinotecan.
Cell Prolif. 2022 Apr;55(4):e13208
NOD/SCID mice
ESCC cell line xenograft models
Intraperitoneal injection
8 mg/kg
Twice a week for 3 weeks
To evaluate the antitumor effect of Irinotecan in ESCC xenograft models, the results showed that Irinotecan significantly inhibited tumor growth, but the effect was inferior to Gimatecan.
Cell Death Dis. 2018 May 31;9(6):661.
Pig
Pig embryos
Embryo injection
5 µM
Single injection, incubated for 6 days
Significantly increased knock-in (KI) frequency in pig embryos without impairing embryo development
Cell Biosci. 2023 Nov 25;13(1):215.
Nude mice
U87 cell subcutaneous xenograft model
Intraperitoneal injection
0.5 mg/kg
Once daily for 5 days, followed by 2 days off
The combination of irinotecan with pitavastatin significantly inhibited tumor growth with lower toxicity.
United States, California
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Jonsson Comprehensive Cancer Center, UCLA
Los Angeles, California, United States, 90095-1781
Wilshire Oncology Medical Group, Inc.
Rancho Cucamonga, California, United States, 91730 收起 <<
United States, Arizona
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Arizona Cancer Center at University of Arizona Health Sciences Center
Tucson, Arizona, United States, 85724-5024 收起 <<
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