General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0LWBKC
ADC Name
CN109069633A ADC-3
Synonyms
CN109069633A_ADC-3
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Organization
Macrogenics Inc.
Drug Status
Investigative
Indication
In total 5 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Lung cancer [ICD11:2C25]
Investigative
Melanoma [ICD11:2C30]
Investigative
Non small cell lung cancer [ICD11:2C25]
Investigative
Ovarian cancer [ICD11:2C73]
Investigative
Drug-to-Antibody Ratio
2
Antibody Name
Anti-human CD276 mAb
 Antibody Info 
Antigen Name
CD276 antigen (CD276)
 Antigen Info 
Payload Name
Undisclosed
Linker Name
CN109069633A ADC-3 linker
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 13 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 12.5
%
CVCL_0479
Ovarian mixed germ cell tumor
Tumor Growth Inhibition value (TGI) 
≈ 25
%
CVCL_0136
Amelanotic melanoma
Tumor Growth Inhibition value (TGI) 
≈ 32.6
%
CVCL_1490
Lung squamous cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 42.3
%
CVCL_0236
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 42.8
%
CVCL_0479
Ovarian mixed germ cell tumor
Tumor Growth Inhibition value (TGI) 
≈ 61.5
%
CVCL_0236
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 65.2
%
CVCL_1490
Lung squamous cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 65.4
%
CVCL_0236
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 75
%
CVCL_0136
Amelanotic melanoma
Tumor Growth Inhibition value (TGI) 
≈ 80
%
CVCL_0136
Amelanotic melanoma
Tumor Growth Inhibition value (TGI) 
≈ 85.7
%
CVCL_0479
Ovarian mixed germ cell tumor
Tumor Growth Inhibition value (TGI) 
≈ 90.9
%
CVCL_0419
Breast adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97.8
%
CVCL_1490
Lung squamous cell carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 9 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
162
pM
CVCL_1511
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
171
pM
CVCL_0236
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
219
pM
CVCL_1490
Lung squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
303
pM
CVCL_0858
Neoplasm
Half Maximal Inhibitory Concentration (IC50) 
735
pM
CVCL_2077
Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
887
pM
CVCL_0132
Amelanotic melanoma
Half Maximal Inhibitory Concentration (IC50) 
0
nM
CVCL_0419
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0
nM
CVCL_0479
Ovarian mixed germ cell tumor
Half Maximal Inhibitory Concentration (IC50) 
0
nM
CVCL_0105
Prostate carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 13 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 12.50% (Day 70) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 1 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model PA-1 CDX model
In Vitro Model Ovarian mixed germ cell tumor PA-1 cells CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 25.00% (Day 49) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 1 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model A375.S2 CDX model
In Vitro Model Amelanotic melanoma A375.S2 cells CVCL_0136
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 32.60% (Day 91) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 1 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model NCI-H1703 CDX model
In Vitro Model Lung squamous cell carcinoma NCI-H1703 cells CVCL_1490
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 42.30% (Day 42) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 1 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model Calu-6 CDX model
In Vitro Model Lung adenocarcinoma Calu-6 cells CVCL_0236
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 42.80% (Day 70) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model PA-1 CDX model
In Vitro Model Ovarian mixed germ cell tumor PA-1 cells CVCL_0479
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 61.50% (Day 42) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model Calu-6 CDX model
In Vitro Model Lung adenocarcinoma Calu-6 cells CVCL_0236
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 65.20% (Day 91) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model NCI-H1703 CDX model
In Vitro Model Lung squamous cell carcinoma NCI-H1703 cells CVCL_1490
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 65.40% (Day 42) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model Calu-6 CDX model
In Vitro Model Lung adenocarcinoma Calu-6 cells CVCL_0236
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 75.00% (Day 49) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model A375.S2 CDX model
In Vitro Model Amelanotic melanoma A375.S2 cells CVCL_0136
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.00% (Day 49) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model A375.S2 CDX model
In Vitro Model Amelanotic melanoma A375.S2 cells CVCL_0136
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.70% (Day 70) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model PA-1 CDX model
In Vitro Model Ovarian mixed germ cell tumor PA-1 cells CVCL_0479
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.90% (Day 79) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model MDA-MB-468 CDX model
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 13 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.80% (Day 91) Positive CD276 expression (CD276+++/++)
Method Description
All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model NCI-H1703 CDX model
In Vitro Model Lung squamous cell carcinoma NCI-H1703 cells CVCL_1490
Revealed Based on the Cell Line Data
Click To Hide/Show 9 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 162.00 pM Positive CD276 expression (CD276+++/++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 171.00 pM Positive CD276 expression (CD276+++/++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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In Vitro Model Lung adenocarcinoma Calu-6 cells CVCL_0236
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 219.00 pM Positive CD276 expression (CD276+++/++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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In Vitro Model Lung squamous cell carcinoma NCI-H1703 cells CVCL_1490
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 303.00 pM Positive CD276 expression (CD276+++/++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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In Vitro Model Neoplasm Hs 700T cells CVCL_0858
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 735.00 pM Positive CD276 expression (CD276+++/++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 887.00 pM Positive CD276 expression (CD276+++/++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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In Vitro Model Amelanotic melanoma A375 cells CVCL_0132
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1.38 nM Positive CD276 expression (CD276+++/++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1.80 nM Positive CD276 expression (CD276+++/++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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In Vitro Model Ovarian mixed germ cell tumor PA-1 cells CVCL_0479
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 2.59 nM Positive CD276 expression (CD276+++/++)
Method Description
Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.

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In Vitro Model Prostate carcinoma DU145 cells CVCL_0105
References
Ref 1 Novel B7-H3- binding molecule, its antibody drug conjugate and its application method.

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