2. Cell Cycle/DNA Damage Autophagy
  3. Topoisomerase Autophagy
  4. Irinotecan hydrochloride

Irinotecan hydrochloride  (Synonyms: (+)-Irinotecan hydrochloride; CPT-11 hydrochloride; VAL-413)

Cat. No.: HY-16562A Purity: 99.89%
Data Sheet
SDS
COA
Handling Instructions Technical Support

Solubility

In Vivo Dissolution Calculator

Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer.

For research use only. We do not sell to patients.

Irinotecan hydrochloride Chemical Structure

Irinotecan hydrochloride Chemical Structure

CAS No. : 100286-90-6

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Based on 50 publication(s) in Google Scholar

Other Forms of Irinotecan hydrochloride:

Irinotecan hydrochloride Related Antibodies

Top Publications Citing Use of Products

48 Publications Citing Use of MCE Irinotecan hydrochloride

WB
IF

    Irinotecan hydrochloride purchased from MedChemExpress. Usage Cited in: J Pharm Pharmacol. 2023 Mar 1;rgad007.  [Abstract]

    Irinotecan (CPT11; 20 μM; 48 h) or Etoposide (VP16; 20 μM; 48 h) induces MDA-MB-231 cells cycle arrest significantly.

    Irinotecan hydrochloride purchased from MedChemExpress. Usage Cited in: Apoptosis. 2016 Feb;21(2):130-42.  [Abstract]

    (a) CPT-11 induces cell cycle arrest and apoptosis in RAW 264.7macrophages. a.Western blot analysis of cleaved caspase-3 and PARP levels. (b) CPT-11 induced cell cycle arrest and apoptosis in mouse peritoneal macrophages. Western blot analysis of cleaved caspase-3 and PARP levels in peritoneal macrophages isolated from vehicleand CPT-11-administered mice. (c) Caspase-3 inhibitor z-DEVD-fmk (ZD) attenuates CPT-11-induced loss of GATA6+ peritoneal macrophages in mice. Western blot analy

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    Topoisomerase Topo I Topo II

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer[1].

    IC50 & Target[1]

    Topoisomerase I

     

    In Vitro

    Irinotecan hydrochloride 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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Irinotecan hydrochloride Related Antibodies
    In Vivo

    Irinotecan hydrochloride (CPT-11 hydrochloride, 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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    NCT NumberSponsorConditionStart DatePhase
    NCT04390399ImmunityBio, Inc.
    Pancreatic Cancer
    		July 21, 2020Phase 2
    NCT03879798Memorial Sloan Kettering Cancer Center
    Small Cell Lung Cancer
    		March 15, 2019Phase 1|Phase 2
    NCT04215159Jin-Hee Ahn|Asan Medical Center
    HER-2 Protein Overexpression|HER-2 Gene Amplification
    		December 30, 2019Phase 2
    Molecular Weight

    623.14

    Formula

    C33H39ClN4O6
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(N1CCC(N2CCCCC2)CC1)OC3=CC=C4N=C5C(CN6C(C(COC([C@@]7(CC)O)=O)=C7C=C65)=O)=C(CC)C4=C3.[H]Cl
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (200.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 3.33 mg/mL (5.34 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 6 mg/mL (9.63 mM); Clear solution

      This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 6 mg/mL (9.63 mM); Clear solution

      This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (16.05 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (16.05 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.89%

    Data Sheet (279 KB) SDS (393 KB)

    COA (251 KB)

    Handling Instructions (2659 KB)
    References
    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.6048 mL 8.0239 mL 16.0478 mL 40.1194 mL
    5 mM 0.3210 mL 1.6048 mL 3.2096 mL 8.0239 mL
    DMSO 10 mM 0.1605 mL 0.8024 mL 1.6048 mL 4.0119 mL
    15 mM 0.1070 mL 0.5349 mL 1.0699 mL 2.6746 mL
    20 mM 0.0802 mL 0.4012 mL 0.8024 mL 2.0060 mL
    25 mM 0.0642 mL 0.3210 mL 0.6419 mL 1.6048 mL
    30 mM 0.0535 mL 0.2675 mL 0.5349 mL 1.3373 mL
    40 mM 0.0401 mL 0.2006 mL 0.4012 mL 1.0030 mL
    50 mM 0.0321 mL 0.1605 mL 0.3210 mL 0.8024 mL
    60 mM 0.0267 mL 0.1337 mL 0.2675 mL 0.6687 mL
    80 mM 0.0201 mL 0.1003 mL 0.2006 mL 0.5015 mL
    100 mM 0.0160 mL 0.0802 mL 0.1605 mL 0.4012 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Irinotecan hydrochloride Related Classifications

    Keywords:

    Irinotecan100286-90-6(+)-IrinotecanCPT-11 VAL-413CPT11CPT 11VAL413VAL 413VAL-413TopoisomeraseAutophagyInhibitorinhibitorinhibit

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