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Irinotecan hydrochloride trihydrate

Catalog No. T0486 CAS 136572-09-3

Synonyms: Irinotecan HCl Trihydrate, CPT-11 HCl Trihydrate

Irinotecan hydrochloride trihydrate (CPT-11 HCl Trihydrate) keeps DNA from unwinding by inhibiting topoisomerase 1.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Irinotecan hydrochloride trihydrate Chemical Structure

Irinotecan hydrochloride trihydrate, CAS 136572-09-3

Pack Size	Availability	Price/USD
25 mg	In stock	$ 36.00
50 mg	In stock	$ 52.00
100 mg	In stock	$ 72.00
200 mg	In stock	$ 96.00
500 mg	In stock	$ 162.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Purity: 99.79%

Purity: 99.78%

Purity: 99.52%

Purity: 98.37%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Irinotecan hydrochloride trihydrate (CPT-11 HCl Trihydrate) keeps DNA from unwinding by inhibiting topoisomerase 1.
In vitro	In the liver, stomach, duodenum, and colon, a single dose of Irinotecan significantly increases the covalent binding of topoisomerase I to DNA. Compared to the control group, there is a marked increase in DNA strand breaks within the colonic mucosal cells in the Irinotecan-treated group. In COLO320 xenografts, Irinotecan induces a 92% maximum growth inhibition.
In vivo	In LoVo and HT-29 cell lines, Irinotecan induces a similar number of cleavable complexes at IC50 concentrations, with no significant difference observed between the two. The formation of cleavable complexes by SN-38 is concentration-dependent and consistent across both cell lines. Notably, intracellular accumulation of Irinotecan differs significantly, with consistently higher levels in HT-29 cells compared to LoVo cells. Carboxylesterase activation of Irinotecan to SN-38 (primarily in the liver) facilitates interaction with its target, topoisomerase I, in plasma, intestines, and tumor tissues. The hydrolysis of Irinotecan’s lactone E-ring and SN-38 is reversible in aqueous solution, with the interconversion of their carboxylate and lactone forms dependent on temperature and pH. For the same concentration of SN-38 glucuronide and Irinotecan in tumor and normal tissues, the yield of SN-38 via β-glucuronidase mediation exceeds that of SN-38 produced from Irinotecan. In SCLC cell lines, Irinotecan exhibits markedly greater activity than in NSCLC cell lines, while tissue histology does not reveal significant differences in SN-38 efficacy.
Cell Research	Exponentially growing cells (LoVo and HT-29 cells) are seeded in 20 cm2 Petri dishes with an optimal cell number for each cell line (2 × 104 for LoVo cells, 105 for HT-29 cells). They are treated 2 days later with increasing concentrations of Irinotecan or SN-38 for one cell doubling time (24 hours for LoVo cells, 40 hours for HT-29 cells). After washing with 0.15 M NaCl, the cells are further grown for two doubling times in normal medium, detached from the support with trypsin-EDTA and counted in a hemocytometer. The IC50 values are then estimated as the Irinotecan or SN-38 concentrations responsible for 50% growth inhibition as compared with cells incubated without Irinotecan or SN-38. (Only for Reference)
Source	Natural Products > Nyssaceae > Camptotheca

Synonyms	Irinotecan HCl Trihydrate, CPT-11 HCl Trihydrate
Molecular Weight	677.18
Formula	C33H45ClN4O9
CAS No.	136572-09-3

Storage

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

Solubility Information

H2O: 1 mg/mL (1.47 mM)

Ethanol: 7 mg/mL (10.33 mM)

DMSO: 93 mg/mL (137.3 mM)

References and Literature

1. Pavillard V, et al. Cancer Chemother Pharmacol. 2002, 49(4), 329-335. 2. Tobin P, et al. Br J Clin Pharmacol. 2006, 62(1), 122-129. 3. Shingyoji M, et al. Cancer Sci. 2004, 95(6), 537-540. 4. van Ark-Otte J, et al. Br J Cancer. 1998, 77(12), 2171-2176. 5. Jansen WJ, et al. Int J Cancer. 1997, 70(3):335-340.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library EMA Approved Drug Library Inhibitor Library Drug Repurposing Compound Library DNA Damage & Repair Compound Library Natural Product Library for HTS Selected Plant-Sourced Compound Library

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Keywords

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