General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0VFGGJ
ADC Name
WO2022078260A1 ADC-5
Synonyms
WO2022078260A1 ADC5
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Organization
Sichuan Baili Pharmaceutical Co., Ltd.
Drug Status
Investigative
Indication
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Drug-to-Antibody Ratio
7.5
Antibody Name
Trastuzumab
 Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
 Antigen Info 
Payload Name
Ln-D5
 Payload Info 
Therapeutic Target
DNA topoisomerase 1 (TOP1)
 Target Info 
Linker Name
WO2022078260A1_ADC-5 linker
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 96
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
2.79
nM
BT-474 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
3.22
nM
MDA-MB-468 cells
Breast adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
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.
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
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 2.79 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.
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) 3.22 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.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
References
Ref 1 Camptothecin derivative and ligand-drug conjugate thereof; 2022-04-21.

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