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Daun02 Cell viability inhibitor,DNA synthisis inhibitor

Catalog No.A3352
Size Price Stock Qty
5mg
$226.00
In stock
10mg
$411.00
In stock
25mg
$642.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Nennig SE, Fulenwider HD, et al. "Selective Lesioning of Nuclear Factor-κB Activated Cells in the Nucleus Accumbens Shell Attenuates Alcohol Place Preference." Neuropsychopharmacology. 2018 Apr;43(5):1032-1040. PMID:28901327
2. Funk D, Coen K, et al. "Role of Central Amygdala Neuronal Ensembles in Incubation of Nicotine Craving. J Neurosci." 2016 Aug 17;36(33):8612-23. PMID:27535909

Quality Control

Quality Control & MSDS

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Chemical structure

Daun02

Related Biological Data

Daun02

Related Biological Data

Daun02

Related Biological Data

Daun02

Biological Activity

Description Daun02 is an inhibitor of cell viability with IC50 values of 1.5 μM, 3.5 μM and 0.5 μM, respectively in Panc02, MCF-7 and T47-D cell lines.
Targets Panc02 MCF-7 T47-D      
IC50 1.5 μM 3.5 μM 0.5 μM      

Protocol

Cell experiment: [1]

Cell lines

Panc02, MCF-7, T47-D, PC3, DU145 and LNCap cells (transduced to express E.coli β-gal)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reacting condition

EC50: 0.5 to 5.5 μM, 24 hours

Applications

The prodrug Daun02 was converted to daunomycin by the β-galactosidase. It inhibited the cell viability with EC50 values of 1.5, 3.5, 0.5, 5.0, 5.5, 5.0 for Panc02, MCF-7, T47-D, PC3, DU145 and LNCap tumor cells, respectively.

Animal experiment: [1]

Animal models

Male athymic BALB/c mice implanted with β-gal-transduced Panc02 cells

Dosage form

Intraperitoneal injection, 200 mg/kg

Application

None of the tumors responded to treatment with intraperitoneal Daun02. The dose for Daun02 was the highest tested due to the limited water solubilityof the compound. At this dose, the animals did not appear to experience anytoxicityas evidenced bynormal physical and behavioral characteristics and continued weight gain. It may be due to the less distribution and the poor penetrability of Daun02 across cell membranes.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] David Farquhar, Bih Fang Pan, Mamoru Sakurai, AjitGhosh, Craig A. Mullen, J. Arly Nelson. Suicide gene therapy using E.Coli β-galactosidase. Cancer ChemotherPharmacol.2002, 50: 65–70.

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Chemical Properties

Cas No. 290304-24-4 SDF Download SDF
Synonyms Daun 02; Daun-02
Chemical Name [3-nitro-4-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]methyl N-[(2S,3S,4S,6R)-6-[(3-acetyl-3,5,12-trihydroxy-10-methoxy-6,11-dioxo-2,4-dihydro-1H-tetracen-1-yl)oxy]-3-hydroxy-2-methyloxan-4-yl]carbamate
Canonical SMILES CC1C(C(CC(O1)OC2CC(CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=O)C)O)NC(=O)OCC6=CC(=C(C=C6)OC7C(C(C(C(O7)CO)O)O)O)[N+](=O)[O-])O
Formula C41H44N2O20 M.Wt 884.79
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
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.

Background

Daun02 is an inhibitor of cell viability with IC50 values of 1.5μM, 3.5μM and 0.5μM, respectively in Panc02, MCF-7 and T47-D cell lines [1].

Daun02, an anthracycline derivative, is a substrate of β-galactosidase. β-galactosidase catalyses Daun02 into daunomycin, which causes apoptotic cell death and blockade of voltagedependent calcium channels. Daun02 has been used in the study of suicide gene therapy which has thepotential to increase the selective toxicityof conventional antitumor agents. In this study, Daun02 is shown to suppress the viability of several β-gal gene transduced tumor celllinesin vitro. However, none of thetumors responded to treatment withDaun02in vivo. This mayhave been due tothe limited aqueous solubilityof the agent.Daun02 is also used to study activated neuronal ensembles in models of conditioned drug effects and relapse. The method is called Daun02 inactivation method. In the Fos–lacZ transgenic rats, the previously drug activated neurons can be inactivated through injection of the prodrug Daun02 [1,2].

References:
[1] David Farquhar, Bih Fang Pan, Mamoru Sakurai, AjitGhosh, Craig A. Mullen, J. Arly Nelson. Suicide gene therapy using E.Coliβ-galactosidase. Cancer ChemotherPharmacol.2002, 50: 65–70.
[2] Fabio C. Cruz, EisukeKoya, Danielle H. Guez-Barber, Jennifer M. Bossert,

Carl R. Lupica, YavinShaham and Bruce T. Hope.New technologies for examining the role of neuronal ensembles in drug addiction and fear.Nature Reviews/Neuroscience. 2013, 14: 743-754.