Irinotecan HCl Trihydrate

Alias: CPT-11 HCl Trihydrate; CPT11;(+)-Irinotecan; Camptosar; CPT-11; CPT 11;Irinophore C; Irinotecan; Irinotecan lactone; Irinotecanum
Cat No.:V1410 Purity: ≥98%
Irinotecan HCl trihydrate (formerly CPT-11;CPT 11;Irinophore C; Irinotecan lactone; Irinotecanum), the hydrochloride salt and trihydrated form of irinotecan which is an antitumor drug and a soluble prodrug of SN-38, is a semisynthetic derivative of camptothecin approved for cancer treatment.
Irinotecan HCl Trihydrate Chemical Structure CAS No.: 136572-09-3
Product category: Topoisomerase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Irinotecan HCl trihydrate (formerly CPT-11; CPT 11; Irinophore C; Irinotecan lactone; Irinotecanum ), the hydrochloride salt and trihydrated form of irinotecan which is an antitumor drug and a soluble prodrug of SN-38, is a semisynthetic derivative of camptothecin approved for cancer treatment. It suppresses P388 leukemia's ability to proliferate with an IC50 value of 3.4μM. Irinotecan was created to prevent toxicity and boost camptothecin's therapeutic effectiveness.

Biological Activity I Assay Protocols (From Reference)
Targets
Topoisomerase I
ln Vitro

Irinotecan hydrochloride trihydrate is an inhibitor of topoisomerase I. Irinotecan causes comparable amounts of cleavable complexes in both LoVo and HT-29 cells, and it inhibits their growth with IC50s of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively[2]. The human umbilical vein endothelial cells' (HUVEC) proliferation is suppressed by irinotecan, with an IC50 of 1.3 μM[3].

ln Vivo
Irinotecan (CPT-11, 5 mg/kg) significantly reduces the growth of tumors when injected intratumorally into rats for five days straight over the course of two weeks. In mice, the same effect is achieved by continuously infusing osmotic minipump fluid intraperitoneally. However, Irinotecan (10 mg/kg) shows no effect on the growth of tumor by i.p[1]. By day 21, it appears that irinotecan (CPT-11, 100–300 mg/kg, i.p.) inhibits the growth of HT-29 xenograft tumors in athymic female mice. Both the Irinotecan (125 mg/kg) plus TSP-1 (10 mg/kg per day) and the Irinotecan (150 mg/kg) plus TSP-1 (20 mg/kg per day) groups are almost as effective as Irinotecan alone, inhibiting tumor growth by 84% and 89%, respectively, at doses of 250 and 300 mg/kg[3].
Cell Assay
In 20 cm2 dishes, exponentially growing cells are seeded with the ideal number of cells for each cell line (20,000 for LoVo cells, 100,000 for HT-29 cells). They receive treatment with irinotecan or SN-38 at increasing concentrations for a single cell doubling period (24 hours for LoVo cells and 40 hours for HT-29 cells) after two days. Following a 0.15 M NaCl wash, the cells are cultured in normal medium for two more doubling times before being separated from the support using trypsin-EDTA and counted using a hemocytometer. Subsequently, the drug concentrations that cause a 50% inhibition of growth in cells treated with the drug are estimated as the IC50 values[2].
Animal Protocol
One cycle of therapy consists of injecting 0.1 cc of the suitable solution intraperitoneally (IV) with irinotecan at a dose of 5 mg/kg per day for 5 days on two consecutive weeks, separated by a 7-day rest period. Over the course of eight weeks, rats receive three cycles. By intratumoral injection, control animals are given 0.1 cc of sterile 0.9% sodium chloride solution according to the same protocol as group II animals[1].
References

[1]. Antitumoral effect of irinotecan (CPT-11) on an experimental model of malignant neuroectodermal tumor. J Neurooncol. 2002 Feb;56(3):219-26.

[2]. Determinants of the cytotoxicity of irinotecan in two human colorectal tumor cell lines. Cancer Chemother Pharmacol. 2002 Apr;49(4):329-35. Epub 2002 Jan 30.

[3]. Thrombospondin-1 plus irinotecan: a novel antiangiogenic-chemotherapeutic combination that inhibits the growth of advanced human colon tumor xenografts in mice. Cancer Chemother Pharmacol. 2004 Mar;53(3):261-6. Epub 2003 Dec 5.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C33H45CLN4O9
Molecular Weight
677.18
Exact Mass
676.29
Elemental Analysis
C, 58.53; H, 6.70; Cl, 5.23; N, 8.27; O, 21.26
CAS #
136572-09-3
Appearance
Yellow solid powder
SMILES
CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)[C@@]4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7.O.O.O.Cl
InChi Key
KLEAIHJJLUAXIQ-JDRGBKBRSA-N
InChi Code
InChI=1S/C33H38N4O6.ClH.3H2O/c1-3-22-23-16-21(43-32(40)36-14-10-20(11-15-36)35-12-6-5-7-13-35)8-9-27(23)34-29-24(22)18-37-28(29)17-26-25(30(37)38)19-42-31(39)33(26,41)4-2;;;;/h8-9,16-17,20,41H,3-7,10-15,18-19H2,1-2H3;1H;3*1H2/t33-;;;;/m0..../s1
Chemical Name
[(19S)-10,19-diethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-7-yl] 4-piperidin-1-ylpiperidine-1-carboxylate;trihydrate;hydrochloride
Synonyms
CPT-11 HCl Trihydrate; CPT11;(+)-Irinotecan; Camptosar; CPT-11; CPT 11;Irinophore C; Irinotecan; Irinotecan lactone; Irinotecanum
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 50~100 mg/mL (73.8~147.7 mM)
Water: <1 mg/mL
Ethanol: ~7 mg/mL (~10.3 mM)
Solubility (In Vivo)
30%Propylene glycol, 5%Tween 80, 65% D5W: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.4767 mL 7.3836 mL 14.7671 mL
5 mM 0.2953 mL 1.4767 mL 2.9534 mL
10 mM 0.1477 mL 0.7384 mL 1.4767 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02192359 Active
Recruiting
Drug: Irinotecan Hydrochloride
Drug: Irinotecan
Recurrent Glioblastoma
Recurrent Gliosarcoma
City of Hope Medical Center March 7, 2016 Phase 1
NCT00045201 Active
Recruiting
Drug: Erlotinib Hydrochloride
Drug: Irinotecan Hydrochloride
Adult Solid Neoplasm National Cancer Institute
(NCI)
June 13, 2002 Phase 1
NCT03290937 Active
Recruiting
Drug: Irinotecan Hydrochloride
Biological: Cetuximab
Metastatic Colorectal Carcinoma
Stage IV Colorectal Cancer
AJCC v8
M.D. Anderson Cancer Center December 27, 2017 Phase 1
NCT03794349 Recruiting Drug: Irinotecan Hydrochloride
Biological: Dinutuximab
High Risk Neuroblastoma
Recurrent Neuroblastoma
Children's Oncology Group July 8, 2019 Phase 2
NCT00576654 Active
Recruiting
Drug: Irinotecan Hydrochloride
Drug: Veliparib
Hodgkin Lymphoma
Non-Hodgkin Lymphoma
National Cancer Institute
(NCI)
December 5, 2007 Phase 1
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