Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0KBUYU
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| ADC Name |
WO2021249228A1 ADC-6
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| Synonyms |
WO2021249228A1 ADC6
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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)
Investigative
Investigative
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| Drug-to-Antibody Ratio |
7.55
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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 |
Undisclosed
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| Linker Name |
WO2021249228A1_ADC-6 linker
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
| Standard Type | Value | Units | Cell Line | Disease Model |
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| Half Maximal Inhibitory Concentration (IC50) |
435.86
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nM
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NCI-N87 cells
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Gastric tubular adenocarcinoma
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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) | ≈ 0.00% (Day 31) | Positive HER2 expression (EPHA2+++/++) | ||
| Method Description |
To establish lung 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 11.25 mg/kg, i.v.
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| In Vivo Model | NCI-H1975 CDX model | ||||
| In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 84.50% (Day 31) | Positive EGFR expression (EGFR+++/++) | ||
| Method Description |
To establish lung 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 3.75 mg/kg, i.v.
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| In Vivo Model | NCI-H1975 CDX model | ||||
| In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.00% (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 3.75 mg/kg, i.v.
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| In Vivo Model | NCI-N87 CDX model | ||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.70% (Day 31) | Positive EGFR expression (EGFR+++/++) | ||
| Method Description |
To establish lung 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 11.25 mg/kg, i.v.
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| In Vivo Model | NCI-H1975 CDX model | ||||
| In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 435.86 nM | Positive HER2 expression (EPHA2+++/++) | ||
| Method Description |
Potency of compounds and ADCs was evaluated using the NCI-N87 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 | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
References
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