General Information of This Peptide-drug Conjugate (PDC)
PDC ID
PDC_00141
PDC Name
DOXoxmCPPamph
PDC Status
Investigative
Indication
In total 1 Indication(s)
Breast cancer
Structure
Peptide Name
oxmCPPamph
 Peptide Info 
Drug Name
Doxorubicin
 Drug Info 
Therapeutic Target
DNA topoisomerase 2-alpha (TOP2A)
 Target Info 
Linker Name
Disulfide bond
 Linker Info 
Formula
C144H205N27O41S2
#Ro5 Violations (Lipinski): 4 Molecular Weight 3034.506
Lipid-water partition coefficient (xlogp) -1.2835
Hydrogen Bond Donor Count (hbonddonor) 25
Hydrogen Bond Acceptor Count (hbondacc) 42
Rotatable Bond Count (rotbonds) 69
Full List of Activity Data of This Peptide-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Breast cancer
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
19 μM
Description
Doxorubicin binds with high affinity to DNA by intercalation, which leads to DNA damage and subsequent growth inhibition44,45. We performed MTT assays in order to determine the viability of the tumor cells and additionally to assess the proliferative potential of the cells after drug treatment. MCF-7 and HT-29 cells were incubated with doxorubicin and the peptide conjugates at various concentrations in the range of 0.1 and 50 μmfor 72 h (in a serum-containing medium), and the results were expressed as IC50-values (Table 1).

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In Vitro Model Colon cancer HT29 cell CVCL_A8EZ
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Breast cancer
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
24.7 μM
Description
Doxorubicin binds with high affinity to DNA by intercalation, which leads to DNA damage and subsequent growth inhibition44,45. We performed MTT assays in order to determine the viability of the tumor cells and additionally to assess the proliferative potential of the cells after drug treatment. MCF-7 and HT-29 cells were incubated with doxorubicin and the peptide conjugates at various concentrations in the range of 0.1 and 50 μmfor 72 h (in a serum-containing medium), and the results were expressed as IC50-values (Table 1).

   Click to Show/Hide
In Vitro Model Colon cancer HT29 cell CVCL_A8EZ
References
Ref 1 Novel cleavable cell-penetrating peptide-drug conjugates: synthesis and characterization. J Pept Sci. 2014 May;20(5):323-33. doi: 10.1002/psc.2617. Epub 2014 Feb 19.