Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0DYMUQ
ADC Name
WO2017059289A1 ADC-108
Synonyms
Thio anti-HER2 hu7C2 LC K149C-52
   Click to Show/Hide
Organization
Genentech, Inc.
Drug Status
Investigative
Indication
In total 1 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Drug-to-Antibody Ratio
1.99
Antibody Name
Thio Anti-HER2 hu7C2 LC K149C
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
Undisclosed
Linker Name
WO2017059289A1_ADC-108 linker
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 5 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 59.94
%
KPL-4 cells
Breast inflammatory carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 84.27
%
KPL-4 cells
Breast inflammatory carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 85.06
%
KPL-4 cells
Breast inflammatory carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 89.73
%
WSU-DLCL2 cells
Diffuse large B-cell lymphoma
Tumor Growth Inhibition value (TGI) 
≈ 95.35
%
KPL-4 cells
Breast inflammatory carcinoma
Obtained from the Model Organism Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 40.52
%
Breast cancer model MMTV-HER2 Fo5
Tumor Growth Inhibition value (TGI) 
≈ 69.41
%
Breast cancer model MMTV-HER2 Fo5
Tumor Growth Inhibition value (TGI) 
≈ 83.57
%
Breast cancer model MMTV-HER2 Fo5
Revealed Based on the Cell Line Data
Click To Hide/Show 8 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
8.46
nM
BJAB cells
Burkitt lymphoma
Half Maximal Inhibitory Concentration (IC50) 
8.96
nM
Jurkat cells
T acute lymphoblastic leukemia
Half Maximal Inhibitory Concentration (IC50) 
11.27
nM
WSU-DLCL2 cells
Diffuse large B-cell lymphoma
Half Maximal Inhibitory Concentration (IC50) 
0.6
ng/mL
SK-BR-3 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
1
ng/mL
KPL-4 cells
Breast inflammatory carcinoma
Half Maximal Inhibitory Concentration (IC50) 
1268.7
ng/mL
BJAB cells
Burkitt lymphoma
Half Maximal Inhibitory Concentration (IC50) 
1342.6
ng/mL
Jurkat cells
T acute lymphoblastic leukemia
Half Maximal Inhibitory Concentration (IC50) 
1689.31
ng/mL
WSU-DLCL2 cells
Diffuse large B-cell lymphoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 59.94% (Day 24) Positive HER2 expression (HER2+++/++)
Method Description
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (0.5 mg/kg) via the tail vein on Day 0.

   Click to Show/Hide
In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 84.27% (Day 24) Positive HER2 expression (HER2+++/++)
Method Description
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (1 mg/kg) via the tail vein on Day 0.

   Click to Show/Hide
In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.06% (Day 24) Positive HER2 expression (HER2+++/++)
Method Description
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (2 mg/kg) via the tail vein on Day 0.

   Click to Show/Hide
In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 89.73% (Day 12) Positive CD22 expression (CD22+++/++)
Method Description
Inoculate 150 mice with WSU-DLCL2 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (2 mg/kg) via the tail vein on Day 0.

   Click to Show/Hide
In Vivo Model WSU-DLCL2 CDX model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 95.35% (Day 24) Positive HER2 expression (HER2+++/++)
Method Description
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (5 mg/kg) via the tail vein on Day 0.

   Click to Show/Hide
In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Obtained from the Model Organism Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 40.52% (Day 7) Positive HER2 expression (HER2+++/++)
Method Description
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 0.5 mg/kg ADC dosing on day 0.
In Vivo Model Breast cancer model MMTV-HER2 Fo5
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.41% (Day 7) Positive HER2 expression (HER2+++/++)
Method Description
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 2 mg/kg ADC dosing on day 0.
In Vivo Model Breast cancer model MMTV-HER2 Fo5
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83.57% (Day 7) Positive HER2 expression (HER2+++/++)
Method Description
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 5 mg/kg ADC dosing on day 0.
In Vivo Model Breast cancer model MMTV-HER2 Fo5
Revealed Based on the Cell Line Data
Click To Hide/Show 8 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 8.46 nM Positive CD22 expression (CD22+++/++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Burkitt lymphoma BJAB cells CVCL_5711
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 8.96 nM Positive CD22 expression (CD22+++/++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model T acute lymphoblastic leukemia Jurkat cells CVCL_0065
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 11.27 nM Positive CD22 expression (CD22+++/++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.60 ng/mL High HER2 expression (HER2 +++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1.00 ng/mL High HER2 expression (HER2+++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1268.70 ng/mL Positive CD22 expression (CD22+++/++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Burkitt lymphoma BJAB cells CVCL_5711
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1342.60 ng/mL Positive CD22 expression (CD22+++/++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model T acute lymphoblastic leukemia Jurkat cells CVCL_0065
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1689.31 ng/mL Positive CD22 expression (CD22+++/++)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
References
Ref 1 Pyrrolobenzodiazepine antibody drug conjugates and methods of use; 2017-04-06.

If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.