Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00309
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| PDC Name |
pHLIP-M-DOX
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Tumor
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| Structure |
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| Peptide Name |
pHLIP (GGEQ)
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Peptide 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 |
Sulfo-SMCC
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Linker Info | ||||
| Peptide Modified Type |
The modification of binding with chemical macromolecules
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| Modified Segment |
Dibenzocyclootyne-maleimide
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| Ternimal Modification |
C-terminal modification
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| Formula |
C233H334N48O70S
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 4959.568 | ||||
| Lipid-water partition coefficient (xlogp) | -9.3618 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 60 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 67 | |||||
| Rotatable Bond Count (rotbonds) | 146 | |||||
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 | Tumor | ||||
| Efficacy Data | Cell viability |
97%
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| Administration Time | 72 h | ||||
| Administration Dosage | 5 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
pHLIP-M-DOX had a negligible effect on HeLa cell proliferation when incubated on cells at either pH at pHLIP concentrations as high as 10 μM. This is consistent with our imaging data that showed no release of DOX into the cell interior at either pH.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
97%
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| Administration Time | 72 h | ||||
| Administration Dosage | 10 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
pHLIP-M-DOX had a negligible effect on HeLa cell proliferation when incubated on cells at either pH at pHLIP concentrations as high as 10 μM. This is consistent with our imaging data that showed no release of DOX into the cell interior at either pH.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
98%
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| Administration Time | 72 h | ||||
| Administration Dosage | 2.5 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
pHLIP-M-DOX had a negligible effect on HeLa cell proliferation when incubated on cells at either pH at pHLIP concentrations as high as 10 μM. This is consistent with our imaging data that showed no release of DOX into the cell interior at either pH.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 4 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
99%
|
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| Administration Time | 72 h | ||||
| Administration Dosage | 5 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
pHLIP-M-DOX had a negligible effect on HeLa cell proliferation when incubated on cells at either pH at pHLIP concentrations as high as 10 μM. This is consistent with our imaging data that showed no release of DOX into the cell interior at either pH.
|
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 5 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
100%
|
|||
| Administration Time | 72 h | ||||
| Administration Dosage | 2.5 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
pHLIP-M-DOX had a negligible effect on HeLa cell proliferation when incubated on cells at either pH at pHLIP concentrations as high as 10 μM. This is consistent with our imaging data that showed no release of DOX into the cell interior at either pH.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
References