Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0MFJAE
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| ADC Name |
wO2023232144A1ADC-1
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| Synonyms |
WO2023232144A1ADC-1
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| Organization |
GeneQuantum Healthcare (Suzhou) Co. Ltd.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
1.93
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| Structure |
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| Antibody Name |
anti-HER2 antibody mAb-1
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
| Payload Name |
WO2023232144A1, ADC-1, Payload
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
WO2023232144A1, ADC-1, linker
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Linker Info | ||||
| Combination Type |
LP-1
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ADC-specific functional property(2027 Update)
Bystander Killing Effect
| Bystander Killing Effect | Description | Reference |
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| no | Undisclosed |
[1]
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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 lnhibition value (TGl) |
115.07
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%
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Undisclosed | Undisclosed |
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 lnhibition value (TGl) | 115.07% | Positive ErbB2/HER2 expression (ErbB2/HER2+++/++) | ||
| Method Description |
In the ErbB2/HER2 high expression NCI-N87 CDX xenograft model, ADC-1 was administered at a dose of 3 mg/kg for five consecutive weeks. Compared with the control group, ADC-1 treatment group displayed significant suppression of tumour growth with an TGI of 115.07 % and T/C of 6.57%.
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| In Vivo Model | High ErbB2/HER2 expression NCI-N87 CDX xenograft model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.04636 nM | Positive ErbB2/HER2 expression (ErbB2/HER2+++/++) | ||
| Method Description |
The ErbB2/HER2 positive cells were cultured overnight with ADC-1 or antibody mAb-1 at different concentrations (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, 0.00051nM) Or different concentrations of MMAE (monomethyloratin E) (30, 10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015nM); The ErbB2/HER2 negative cells cultured overnight were added with ADC-1 or antibody mAb-1 at different concentrations (100, 10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015nM) Or different concentrations of MMAE (30, 10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015nM); Puromycin with a final concentration of 5uM was added to the control group. Continue warming at 37°C for 72~120h. 3) Remove the cell plates from the 37°C cell incubator and balance for about 30 minutes to room temperature. Each well is supplemented with 100uLCellTiter Glo reagent, the oscillator oscillates for 2min and then stands at room temperature for 10min away from light. The luminescence value (RLU) is measured.
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| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | 0.08706 nM | Positive ErbB2/HER2 expression (ErbB2/HER2+++/++) | ||
| Method Description |
The ErbB2/HER2 positive cells were cultured overnight with ADC-1 or antibody mAb-1 at different concentrations (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, 0.00051nM) Or different concentrations of MMAE (monomethyloratin E) (30, 10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015nM); The ErbB2/HER2 negative cells cultured overnight were added with ADC-1 or antibody mAb-1 at different concentrations (100, 10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015nM) Or different concentrations of MMAE (30, 10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015nM); Puromycin with a final concentration of 5uM was added to the control group. Continue warming at 37°C for 72~120h. 3) Remove the cell plates from the 37°C cell incubator and balance for about 30 minutes to room temperature. Each well is supplemented with 100uLCellTiter Glo reagent, the oscillator oscillates for 2min and then stands at room temperature for 10min away from light. The luminescence value (RLU) is measured.
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References