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Irinotecan HCl Trihydrate

TOPO 1 inhibitor CAS# 136572-09-3

Irinotecan HCl Trihydrate

Catalog No. BCC5091----Order now to get a substantial discount!

Product Name & Size Price Stock
Irinotecan HCl Trihydrate:10mg $54.00 In stock
Irinotecan HCl Trihydrate:20mg $92.00 In stock
Irinotecan HCl Trihydrate:50mg $216.00 In stock
Irinotecan HCl Trihydrate:100mg $378.00 In stock
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Quality Control of Irinotecan HCl Trihydrate

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Chemical structure

Irinotecan HCl Trihydrate

3D structure

Chemical Properties of Irinotecan HCl Trihydrate

Cas No. 136572-09-3 SDF Download SDF
PubChem ID 60837 Appearance Powder
Formula C33H45ClN4O9 M.Wt 677.18
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 50 mg/mL (73.84 mM; Need ultrasonic)
H2O : 1.52 mg/mL (2.24 mM; Need ultrasonic and warming)
SMILES CCC1=C2C=C(C=CC2=NC3=C1CN4C3=CC5=C(C4=O)COC(=O)C5(CC)O)OC(=O)N6CCC(CC6)N7CCCCC7.O.O.O.Cl
Standard InChIKey KLEAIHJJLUAXIQ-JDRGBKBRSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Irinotecan HCl Trihydrate

DescriptionIrinotecan hydrochloride trihydrate is a water soluble topoisomerase I inhibitor with antitumor activity.In Vitro:Irinotecan hydrochloride trihydrate is a topoisomerase I inhibitor. Irinotecan inhibits the growth of LoVo and HT-29 cells, with IC50s of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively, and induces similar amounts of cleavable complexes in both in LoVo and HT-29 cells[2]. Irinotecan suppresses the proliferation of human umbilical vein endothelial cells (HUVEC), with an IC50 of 1.3 μM[3].In Vivo:Irinotecan (CPT-11, 5 mg/kg) significantly inhibits the growth of tumors by intratumoral injection daily for 5 days, on two consecutive weeks in rats, and such effects also occur via continuous intraperitoneal infusion by osmotic minipump into mice. However, Irinotecan (10 mg/kg) shows no effect on the growth of tumor by i.p[1]. Irinotecan (CPT-11, 100-300 mg/kg, i.p.) apparently suppresses tumor growth of HT-29 xenografts in athymic female mice by day 21. The two groups of Irinotecan (125 mg/kg) plus TSP-1 (10 mg/kg per day) or Irinotecan (150 mg/kg) in combination TSP-1 (20 mg/kg per day) are nearly equally effective and inhibit tumor growth 84% and 89%, respectively, and both are more effective than Irinotecan alone at doses of 250 and 300 mg/kg[3].

References:
[1]. Morales C, et al. Antitumoral effect of irinotecan (CPT-11) on an experimental model of malignant neuroectodermal tumor. J Neurooncol. 2002 Feb;56(3):219-26. [2]. Pavillard V, et al. 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]. Allegrini G, et al. 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.

Protocol

Cell Assay [2]
Exponentially growing cells are seeded in 20 cm2 dishes with an optimal cell number for each cell line (20,000 for LoVo cells, 100,000 for HT-29 cells). They are treated 2 days later with increasing concentrations of irinotecan or SN-38 for one cell doubling time (24 h for LoVo cells, 40 h 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 drug concentrations responsible for 50% growth inhibition as compared with cells incubated without drug[2].

Animal Administration [1]
Irinotecan has been administered by intratumoral injection at 0.1 cc volume of the appropriate solution, for a doses of 5 mg/kg daily for 5 days, on two consecutive weeks, followed by a 7-days rest period, referred to as one cycle of therapy. Rats receive three cycles over a period of 8 weeks. Control animals receive 0.1 cc of sterile 0.9% sodium chloride solution by intratumoral injection in the same rule of administration as that of animals of group II[1].

References:
[1]. Morales C, et al. Antitumoral effect of irinotecan (CPT-11) on an experimental model of malignant neuroectodermal tumor. J Neurooncol. 2002 Feb;56(3):219-26. [2]. Pavillard V, et al. 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]. Allegrini G, et al. 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.

Irinotecan HCl Trihydrate Dilution Calculator

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Irinotecan HCl Trihydrate Molarity Calculator

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Preparing Stock Solutions of Irinotecan HCl Trihydrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.4767 mL 7.3836 mL 14.7671 mL 29.5342 mL 36.9178 mL
5 mM 0.2953 mL 1.4767 mL 2.9534 mL 5.9068 mL 7.3836 mL
10 mM 0.1477 mL 0.7384 mL 1.4767 mL 2.9534 mL 3.6918 mL
50 mM 0.0295 mL 0.1477 mL 0.2953 mL 0.5907 mL 0.7384 mL
100 mM 0.0148 mL 0.0738 mL 0.1477 mL 0.2953 mL 0.3692 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Irinotecan HCl Trihydrate

Irinotecan HCl Trihydrate (CPT-11) is a semisynthetic derivative of camptothecin with IC50 value of 3.4μM in P388 leukemia [1].

CPT-11 is synthesized to avoid toxicity and to improve therapeutic efficacy of camptothecin. It has been approved by FDA for the treatment of patients with metastatic carcinoma of the colon or rectum whose disease has recurred or progressed following 5-fluorouracil-based therapy. CPT-11 is a soluble prodrug of SN-38, it is converted into SN-38 by carboxylesterase enzymes in vivo. SN-38 is a potent inhibitor of topoisomerase I [2].

CPT-11 is found to have efficacy against drug-resistant as well as drug-sensitive tumor cells. It inhibits the growth of the tumors which are VCR- resistant or ADM-resistant. The inhibition can also occur in VCR- and ADM-resistant tumor bearing mice [1].

References:
[1] Tsuruo T, Matsuzaki T, Matsushita M, Saito H, Yokokura T. Antitumor effect of CPT-11, a new derivative of camptothecin, against pleiotropic drug-resistant tumors in vitro and in vivo. Cancer Chemother Pharmacol. 1988;21(1):71-4.
[2] Slatter JG, Schaaf LJ, Sams JP, Feenstra KL, Johnson MG, Bombardt PA, Cathcart KS, Verburg MT, Pearson LK, Compton LD, Miller LL, Baker DS, Pesheck CV, Lord RS 3rd. Pharmacokinetics, metabolism, and excretion of irinotecan (CPT-11) following I.V. infusion of [(14)C]CPT-11 in cancer patients. Drug Metab Dispos. 2000 Apr;28(4):423-33.

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Description

Irinotecan hydrochloride trihydrate is a topoisomerase I inhibitor with antitumor activity.

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