Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0YSXXF
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| ADC Name |
Pyro-Linker-ZHER2
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| Synonyms |
Pyro Linker ZHER2
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| Drug Status |
Investigative
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| Indication |
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
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| Antibody Name |
Modified ZHER2:2891 protein (ZHER2)
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
| Payload Name |
Pyropheophorbide-a
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Payload Info | ||||
| Linker Name |
Pyro-Linker based linker
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
| Standard Type | Value | Units | Cell Line | Disease Model |
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| Tumor Growth Inhibition value (TGI) |
≈ 100
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%
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NCI-N87 cells
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Gastric tubular adenocarcinoma
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Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 19) | High HER2 expression (HER2 +++) | ||
| Method Description |
BALB/c nude mice bearing HER2-high expression NCI-N87 tumors received iv injection of 20 nmol/mouse of Pyro-Linker-ZHER2, Pyro-Linker-OH, Pyro, or PBS buffer only and then irradiated with 180 J/cm2 light 4 h (for groups of PyroLinker-ZHER2 and PBS buffer only) postinjection.
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| In Vivo Model | NCI-N87 CDX model | ||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 12.50 nM | High HER2 expression (HER2 +++) | ||
| Method Description |
Dark toxicity was measured without light illumination, and a HER2 receptor blocking experiment was carried out by preincubation of the cells with free ZHER2:2891 affibody (10.0 M) for 4 h before the addition of Pyro, Pyro-Linker-OH, or Pyro-Linker-ZHER2.
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 23.00 nM | High HER2 expression (HER2 +++) | ||
| Method Description |
Dark toxicity was measured without light illumination, and a HER2 receptor blocking experiment was carried out by preincubation of the cells with free ZHER2:2891 affibody (10.0 M) for 4 h before the addition of Pyro, Pyro-Linker-OH, or Pyro-Linker-ZHER2.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Low HER2 expression (HER2 -) | ||
| Method Description |
Dark toxicity was measured without light illumination, and a HER2 receptor blocking experiment was carried out by preincubation of the cells with free ZHER2:2891 affibody (10.0 M) for 4 h before the addition of Pyro, Pyro-Linker-OH, or Pyro-Linker-ZHER2.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Low HER2 expression (HER2 -) | ||
| Method Description |
Dark toxicity was measured without light illumination, and a HER2 receptor blocking experiment was carried out by preincubation of the cells with free ZHER2:2891 affibody (10.0 M) for 4 h before the addition of Pyro, Pyro-Linker-OH, or Pyro-Linker-ZHER2.
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| In Vitro Model | Prostate carcinoma | PC-3 cells | CVCL_0035 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | High HER2 expression (HER2 +++) | ||
| Method Description |
Dark toxicity was measured without light illumination, and a HER2 receptor blocking experiment was carried out by preincubation of the cells with free ZHER2:2891 affibody (10.0 M) for 4 h before the addition of Pyro, Pyro-Linker-OH, or Pyro-Linker-ZHER2.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells (blocking) | CVCL_1603 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | Low HER2 expression (HER2 -) | ||
| Method Description |
Dark toxicity was measured without light illumination, and a HER2 receptor blocking experiment was carried out by preincubation of the cells with free ZHER2:2891 affibody (10.0 M) for 4 h before the addition of Pyro, Pyro-Linker-OH, or Pyro-Linker-ZHER2.
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| In Vitro Model | Prostate carcinoma | PC-3 cells (blocking) | CVCL_0035 | ||
References
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