2. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  3. Topoisomerase ADC Cytotoxin
  4. Daun02

Daun02 is a proagent of the topoisomerase inhibitor Daunorubicin.

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

Daun02 Chemical Structure

Daun02 Chemical Structure

CAS No. : 290304-24-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 514 In-stock
Solution
10 mM * 1 mL in DMSO USD 514 In-stock
Solid
2 mg USD 216 In-stock
5 mg USD 290 In-stock
10 mg USD 528 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

Daun02 Related Antibodies

Top Publications Citing Use of Products

    Daun02 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Jan 3;7:39817.  [Abstract]

    Photomicrographs represent cFos in the MePD after Meth and hormone administration following DAUN02 or vehicle infusions. A student’s t-test show DAUN02 significantly reduces Fos-ir cells in the MePD compared to the vehicle-treated cohort.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Daun02 is a proagent of the topoisomerase inhibitor Daunorubicin.

    IC50 & Target[2]

    Topoisomerase

     

    Daunorubicins/Doxorubicins

     

    In Vitro

    Daun02 is a prodrug, which is converted by β-galactosidase to Daunorubicin, which has been shown to reduce calcium ion (Ca2+)-dependent action potentials in neuroblastoma cells[1]. Daunorubicin is a topoisomerase inhibitor[2]. Daun02 is a good substrate for β-galactosidase (β-gal). The concentration of Daun02 producing 50% (EC50) decrease in cell viability is 0.5 μM, 1.5 μM, and 3.5 μM for T47-D, Panc02, and MCF-7, respectively[3].

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

    Daun02 Related Antibodies
    In Vivo

    Daun02 is a good substrate for β-gal with Km and Vmax values of 0.37 mM and 8.6 μmol/min/mg protein. At a concentration of 10-5 M, Daun02 is 79% bound to plasma protein compares to 94% for Daunomycin[3].

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

    884.79

    Formula

    C41H44N2O20
    CAS No.
    Appearance

    Solid

    Color

    Brown to wine

    SMILES

    O[C@H]1[C@H](O[C@H]([C@@H]([C@H]1O)O)OC2=CC=C(C=C2[N+]([O-])=O)COC(N[C@@H]3[C@@H]([C@@H](O[C@H](C3)O[C@H]4C[C@](C(C)=O)(CC5=C(C(C(C6=C7C(OC)=CC=C6)=O)=C(C(O)=C54)C7=O)O)O)C)O)=O)CO
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (113.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1302 mL 5.6511 mL 11.3021 mL
    5 mM 0.2260 mL 1.1302 mL 2.2604 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 2.5 mg/mL (2.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    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, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.72%

    COA (253 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [3]

    Murine Panc02 cells are maintained as exponentiallygrowing monolayer cultures in DMEM/F12 or RPMI-1640 medium supplemented with 10% FBS, 1% glutamine, penicillin, and streptomycin at 37°C. For cytotoxicity assay, the cells are seeded into 96-well microplates and incubated overnight. Initial experiments indicate that FBS contains low levels of intrinsic β-gal activity as evidenced by the slow conversion of Daun02 to Daunomycin; however, this is not evident for human serum. Therefore, prior to addition of Daun02, the FBS concentration is reduced from 10% to 1% for Panc02 cells. Human serum (10%) is used for the transduced human cell lines. The cells are incubated for 24 h and then MTT is added. Lysis buffer (20% SDS dissolved in 50% DMF) is added 4 h after the addition of MTT and the cells are incubated overnight. The optical density at 570 nm is determined using a BIO-RAD microplate reader. Cytotoxicity is expressed as the concentration of drug or prodrug that produced a 50% (EC50) reduction in cell viability[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice[3]
    Male athymic BALB/c mice (nu/nu genotype, 18-20 g) are used. Daunomycin is administered at a dose of 20 mg/kg in 100 μL normal saline solution into the tail vein. Daun02 is administered intraperitoneallyat a dose of 200 mg/kg in 200 μL vehicle. (This route is selected because the volume of drug solution, 200 μL, is too great for tail vein administration.) Tumor volume is determined bycaliper measurement in two dimensions and converted to tumor mass. Tumor growth is monitored over a period of 30 days or until the tumors has reached a mass of 5% of bodyweight (about 1 g). The animals are then killed bycarbon dioxide asphyxiation.

    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. 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
    DMSO 1 mM 1.1302 mL 5.6511 mL 11.3021 mL 28.2553 mL
    5 mM 0.2260 mL 1.1302 mL 2.2604 mL 5.6511 mL
    10 mM 0.1130 mL 0.5651 mL 1.1302 mL 2.8255 mL
    15 mM 0.0753 mL 0.3767 mL 0.7535 mL 1.8837 mL
    20 mM 0.0565 mL 0.2826 mL 0.5651 mL 1.4128 mL
    25 mM 0.0452 mL 0.2260 mL 0.4521 mL 1.1302 mL
    30 mM 0.0377 mL 0.1884 mL 0.3767 mL 0.9418 mL
    40 mM 0.0283 mL 0.1413 mL 0.2826 mL 0.7064 mL
    50 mM 0.0226 mL 0.1130 mL 0.2260 mL 0.5651 mL
    60 mM 0.0188 mL 0.0942 mL 0.1884 mL 0.4709 mL
    80 mM 0.0141 mL 0.0706 mL 0.1413 mL 0.3532 mL
    100 mM 0.0113 mL 0.0565 mL 0.1130 mL 0.2826 mL
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    Daun02 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Daun02290304-24-4Daun 02Daun-02TopoisomeraseADC CytotoxinADC PayloadInhibitorinhibitorinhibit

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