1. Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
  2. Topoisomerase
    ADC Cytotoxin

Daun02 

Cat. No.: HY-13061 Purity: 98.56%
Handling Instructions

Daun02 is converted by β-galactosidase to Daunorubicin, which is a topoisomerase inhibitor.

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
10 mM * 1 mL in DMSO USD 514 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
2 mg USD 216 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 290 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 528 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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    Daun02 purchased from MCE. Usage Cited in: Sci Rep. 2017 Jan 3;7:39817.

    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.

    View All Topoisomerase Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Daun02 is converted by β-galactosidase to Daunorubicin, which is a topoisomerase inhibitor.

    IC50 & Target[2]

    Topoisomerase

     

    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].

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.1130 mL 0.5651 mL 1.1302 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [3]

    Daun02 is dissolved in DMSO and stored, and then diluted with appropriate media before use[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]

    Daun02 is formulated in normal saline containing 10% DMSO and 10% Emulfur (Mice)[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
    Molecular Weight

    884.79

    Formula

    C₄₁H₄₄N₂O₂₀

    CAS No.

    290304-24-4

    SMILES

    O[[email protected]]1[[email protected]](O[[email protected]]([[email protected]@H]([[email protected]]1O)O)OC2=CC=C(C=C2[N+]([O-])=O)COC(N[[email protected]@H]3[[email protected]@H]([[email protected]@H](O[[email protected]](C3)OC4CC(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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    Daun02
    Cat. No.:
    HY-13061
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