Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00049
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| PDC Name |
DT7-SS-DOX
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| PDC Status |
Investigative
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| Indication |
In total 3 Indication(s)
Glioblastoma
Hepatoblastoma
Lung adenocarcinoma
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| Structure |
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| Peptide Name |
DT7
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Peptide Info | ||||
| Receptor Name |
Transferrin receptor protein 1 (TFRC)
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Receptor Info | ||||
| Drug Name |
Doxorubicin
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Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 2-alpha (TOP2A)
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Target Info | ||||
| Linker Name |
SPDP
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Linker Info | ||||
| Peptide Modified Type |
Amino acid modifications
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| Modified Segment |
D-amino acids
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| Ternimal Modification |
C-terminal modification
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| Formula |
C74H96N16O22S2
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| #Ro5 Violations (Lipinski): 4 | Molecular Weight | 1625.806 | ||||
| Lipid-water partition coefficient (xlogp) | -1.7585 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 19 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 27 | |||||
| Rotatable Bond Count (rotbonds) | 40 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Glioblastoma | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.70 ± 0.22 µM
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| Administration Time | 48 h | ||||
| Evaluation Method | CCK-8 assay | ||||
| MOA of PDC |
Both conjugates exhibited targeted antiproliferative effects on TfR overexpressed tumor cells and little toxicity to TfR low-expressed normal cells compared with free DOX. Moreover, the DT7-SS-DOX conjugate possessed higher serum stability, more sustained reduction-triggered drug release characteristics, and stronger in vitro antiproliferative activity as compared to LT7-SS-DOX.
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| Description |
DT7-SS-DOX exhibited good in vitro antiproliferative activity against the three tumor cell lines, with IC50 values of 5.70 ± 0.22 μM (U87), 7.01 ± 1.64 μM (HepG2), and 20.61 ± 4.81 μM (A549), respectively.
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| In Vitro Model | Glioblastoma | U87 cell | CVCL_3429 | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Hepatoblastoma | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
7.01 ± 1.64 µM
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| Administration Time | 48 h | ||||
| Evaluation Method | CCK-8 assay | ||||
| MOA of PDC |
Both conjugates exhibited targeted antiproliferative effects on TfR overexpressed tumor cells and little toxicity to TfR low-expressed normal cells compared with free DOX. Moreover, the DT7-SS-DOX conjugate possessed higher serum stability, more sustained reduction-triggered drug release characteristics, and stronger in vitro antiproliferative activity as compared to LT7-SS-DOX.
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| Description |
DT7-SS-DOX exhibited good in vitro antiproliferative activity against the three tumor cell lines, with IC50 values of 5.70 ± 0.22 μM (U87), 7.01 ± 1.64 μM (HepG2), and 20.61 ± 4.81 μM (A549), respectively.
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| In Vitro Model | Hepatoblastoma | Hep-G2 cell | CVCL_0027 | ||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Lung adenocarcinoma | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
20.61 ± 4.81 µM
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| Administration Time | 48 h | ||||
| Evaluation Method | CCK-8 assay | ||||
| MOA of PDC |
Both conjugates exhibited targeted antiproliferative effects on TfR overexpressed tumor cells and little toxicity to TfR low-expressed normal cells compared with free DOX. Moreover, the DT7-SS-DOX conjugate possessed higher serum stability, more sustained reduction-triggered drug release characteristics, and stronger in vitro antiproliferative activity as compared to LT7-SS-DOX.
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|
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| Description |
DT7-SS-DOX exhibited good in vitro antiproliferative activity against the three tumor cell lines, with IC50 values of 5.70 ± 0.22 μM (U87), 7.01 ± 1.64 μM (HepG2), and 20.61 ± 4.81 μM (A549), respectively.
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| In Vitro Model | Lung adenocarcinoma | A-549 cell | CVCL_0023 | ||
| Experiment 4 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Glioblastoma | ||||
| Efficacy Data | Proliferation inhibitory activity |
95.10%
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| Administration Time | 48 h | ||||
| Evaluation Method | CCK-8 assay | ||||
| MOA of PDC |
Both conjugates exhibited targeted antiproliferative effects on TfR overexpressed tumor cells and little toxicity to TfR low-expressed normal cells compared with free DOX. Moreover, the DT7-SS-DOX conjugate possessed higher serum stability, more sustained reduction-triggered drug release characteristics, and stronger in vitro antiproliferative activity as compared to LT7-SS-DOX.
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| Description |
The proliferation inhibitory activity of LT7-SS-DOX was the weakest among the three drugs because the cell viabilities of U87, HepG2, and A549 cells after incubation with LT7-SS-DOX (equal DOX concentration of 20 μM) for 48 h were 95.1%, 73.1%, and 83.2%, respectively.
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| In Vitro Model | Glioblastoma | U87 cell | CVCL_3429 | ||
References