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| 100mg |
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| 250mg |
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| 500mg |
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Irinotecan hydrochloride (also known as CPT-11; (+)-Irinotecan) is a potent topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. Camptothecin, a quinoline-based alkaloid that is cytotoxic and extracted from the Asian tree Camptotheca acuminata, is the semisynthetic derivative of irenotecan hydrochloride. Irinotecan is a prodrug that requires the conversion of a carboxylesterase-converting enzyme to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38). Compared to its parent compound, irinotecan, SN-38 has 1000 times greater potency.
| Targets |
cytotoxicity in LoVo cells ( IC50 = 15.8 μM ); cytotoxicity in HT-29 cells ( IC50 = 5.17 μM ); Topo I
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| ln Vitro |
Irinotecan and Gefitinibstudies have also linked to significantly reduce MDA-MB-231 cell migration and proliferation.[2]
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| ln Vivo |
When treating TNBC subtype cells in a xenograft model, gefitinib and irinotecan work synergistically very well.[/2]
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| 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. The drug concentrations that cause a 50% inhibition in growth when compared to cells cultured without the drug are then estimated to be the IC50 values.
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| Animal Protocol |
One cycle of therapy consists of five days of 5 mg/kg of iminotecan administered intraperitoneally (IV) at a volume of 0.1 cc of the suitable solution, on two separate weeks. The administration of the medication is followed by a seven-day rest period. In an eight-week period, rats receive three cycles. Under the same intratumoral injection guidelines as group II animals, control animals receive 0.1 cc of sterile 0.9% sodium chloride solution.
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| References |
| Molecular Formula |
C₃₃H₃₉CLN₄O₆
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|---|---|
| Molecular Weight |
623.14
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| Exact Mass |
622.26
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| Elemental Analysis |
C, 63.61; H, 6.31; Cl, 5.69; N, 8.99; O, 15.40
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| CAS # |
100286-90-6
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| Related CAS # |
136572-09-3 (HCl trihydrate); 1329502-92-2 (Carboxylate Sodium Salt); 143490-53-3 (Lactone Impurity); 100286-90-6 (HCl); 97682-44-5 (Free base)
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| Appearance |
Solid powder
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| SMILES |
CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)[C@@]4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7.Cl
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| InChi Key |
GURKHSYORGJETM-WAQYZQTGSA-N
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| InChi Code |
InChI=1S/C33H38N4O6.ClH/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/t33-;/m0./s1
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| 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;hydrochloride
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| Synonyms |
CPT-11 hydrochloride; Camptothecin 11 hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100~125 mg/mL (160.5~200.6 mM)
H2O: ~3.3 mg/mL (~5.3 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5%DMSO+ 40%PEG300+ 5%Tween 80+ 50%ddH2O: 5.0mg/ml (8.02mM) Solubility in Formulation 5: 10 mg/mL (16.05 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 6: 10 mg/mL (16.05 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6048 mL | 8.0239 mL | 16.0478 mL | |
| 5 mM | 0.3210 mL | 1.6048 mL | 3.2096 mL | |
| 10 mM | 0.1605 mL | 0.8024 mL | 1.6048 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.
Calculation results
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.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04074343 | Active Recruiting |
Drug: TAS-102 Drug: Irinotecan |
Gastric Adenocarcinoma GastroEsophageal Cancer |
University of California, Irvine | August 26, 2019 | Phase 1 |
| NCT04641871 | Active Recruiting |
Drug: Irinotecan Hydrochloride Drug: Sym021 |
Metastatic Cancer Solid Tumor |
Symphogen A/S | October 12, 2020 | Phase 1 |
| NCT03567629 | Active Recruiting |
Drug: Irinotecan Drug: Oxaliplatin |
mCRC | Peking University | May 29, 2018 | Phase 2 |
| NCT03323034 | Active Recruiting |
Drug: Irinotecan Drug: Pevonedistat |
Recurrent Lymphoma Refractory Lymphoma |
Children's Oncology Group | January 11, 2018 | Phase 1 |
| NCT03365882 | Active Recruiting |
Drug: Irinotecan Hydrochloride Biological: Cetuximab |
Colon Adenocarcinoma Rectal Adenocarcinoma |
SWOG Cancer Research Network | November 27, 2017 | Phase 2 |
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