Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0ICMWF
ADC Name
WO2020063673A1 ADC-1
Synonyms
WO2020063673A1_ADC 1
   Click to Show/Hide
Organization
Jiangsu Hengrui Pharmaceuticals Co., Ltd.
Drug Status
Investigative
Indication
In total 6 Indication(s)
Astrocytoma [ICD11:2F36]
Investigative
Colon cancer [ICD11:2B90]
Investigative
Esophageal cancer [ICD11:2B70]
Investigative
Kidney cancer [ICD11:2C90-2C91]
Investigative
Melanoma [ICD11:2C30]
Investigative
Non-small cell lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
7.5
Structure
Antibody Name
Anti-CD276 mAb h1702DS
  Antibody Info 
Antigen Name
CD276 antigen (CD276)
  Antigen Info 
Payload Name
Undisclosed
Linker Name
WO2020063673A1_ADC-1 linker
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 40.85
%
Detroit 562 cells
Pharyngeal squamous cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 62.55
%
Detroit 562 cells
Pharyngeal squamous cell carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
23.72
nM
A-375 cells
Amelanotic melanoma
Half Maximal Inhibitory Concentration (IC50) 
26.54
nM
Calu-6 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
26.9
nM
Detroit 562 cells
Pharyngeal squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
29
nM
U-87MG cells
Glioblastoma
Half Maximal Inhibitory Concentration (IC50) 
196.6
nM
A498 cells
Renal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 500
nM
CHO-K1 cells
Normal
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 40.85% (Day 28) Positive CD276 expression (CD276 +++/++)
Method Description
Conjugates of the exemplary antibodies were tested using an established xenograft model of Detroit562 cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1mpk, QW*3 of one of the conjugates listed above or with PBS only.
In Vivo Model Detroit 562 CDX model
In Vitro Model Pharyngeal squamous cell carcinoma Detroit 562 cells CVCL_1171
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 62.55% (Day 28) Positive CD276 expression (CD276 +++/++)
Method Description
Conjugates of the exemplary antibodies were tested using an established xenograft model of Detroit562 cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3mpk, QW*3 of one of the conjugates listed above or with PBS only.
In Vivo Model Detroit 562 CDX model
In Vitro Model Pharyngeal squamous cell carcinoma Detroit 562 cells CVCL_1171
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 23.72 nM Positive CD276 expression (CD276 +++/++)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Amelanotic melanoma A-375 cells CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 26.54 nM Positive CD276 expression (CD276 +++/++)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
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) 26.90 nM Positive CD276 expression (CD276 +++/++)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Pharyngeal squamous cell carcinoma Detroit 562 cells CVCL_1171
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 29.00 nM Positive CD276 expression (CD276 +++/++)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Glioblastoma U-87MG cells CVCL_0022
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 196.60 nM Positive CD276 expression (CD276 +++/++)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Renal carcinoma A498 cells CVCL_1056
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500 nM Negative CD276 expression (CD276 -)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Normal CHO-K1 cells CVCL_0214
References
Ref 1 Anti-b7h3 antibody-exatecan analog conjugate and medicinal use thereof; 2020-04-02.

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