Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
ADC ID |
DRG0AQDHE
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ADC Name |
WO2022078260A1 ADC-2
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Synonyms |
WO2022078260A1 ADC2
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Organization |
Sichuan Baili Pharmaceutical Co., Ltd.
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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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Drug-to-Antibody Ratio |
7.4
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Antibody Name |
Trastuzumab
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Antibody Info | ||||
Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
Payload Name |
Ln-D1
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Payload Info | ||||
Therapeutic Target |
DNA topoisomerase 1 (TOP1)
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Target Info | ||||
Linker Name |
WO2022078260A1_ADC-2 linker
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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) |
≈ 96
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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) | ≈ 96.00% (Day 31) | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
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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) | 29.01 nM | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 52.21 nM | Positive HER2 expression (EPHA2+++/++) | ||
Method Description |
Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
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In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 |
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