Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0GSKME
ADC Name
Cet-TPL
Synonyms
Cet TPL; Cet-TPL conjugate
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 2 Indication(s)
Head and neck squamous carcinoma [ICD11:2C31]
Investigative
Non-small cell lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
5.5
Antibody Name
Cetuximab
  Antibody Info 
Antigen Name
Epidermal growth factor receptor (EGFR)
  Antigen Info 
Payload Name
Triptolide
  Payload Info 
Therapeutic Target
Nuclear factor NF-kappa-B p105 subunit (NFKB1)
  Target Info 
Linker Name
N-hydroxysuccinimide based linker
  Linker Info 
Conjugate Type
Random conjugation through nucleophilic lysines.
General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 72.17
%
Lung adenocarcinoma PDX model (PDX: PDX1)
Tumor Growth Inhibition value (TGI) 
≈ 91.89
%
Lung adenocarcinoma PDX model (PDX: PDX1)
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 12.39
%
NCI-H520 cells
Lung squamous cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 64
%
A-549 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 93.8
%
UM-SCC-6 cells
Squamous cell carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
6.25 ug/mL - 12.50 ug/mL
ug/mL
UM-SCC-6 cells
Squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
12.5
ug/mL
A-549 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
12.5
ug/mL
NCI-H1299 cells
Lung large cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 100
ug/mL
NCI-H520 cells
Lung squamous cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-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) ≈ 72.17% (Day 13) Positive EGFR expression (EGFR +++/++)
Method Description
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model Lung adenocarcinoma PDX model (PDX: PDX1)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 91.89% (Day 15) Positive EGFR expression (EGFR +++/++)
Method Description
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model Lung adenocarcinoma PDX model (PDX: PDX1)
Discovered Using Cell Line-derived Xenograft Model
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) ≈ 12.39% (Day 15) Negative EGFR expression (EGFR -)
Method Description
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model H520 CDX model
In Vitro Model Lung squamous cell carcinoma NCI-H520 cells CVCL_1566
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 64.00% (Day 18) Positive EGFR expression (EGFR +++/++)
Method Description
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model A549 CDX model
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 93.80% (Day 24) Positive EGFR expression (EGFR +++/++)
Method Description
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model SCC6 CDX model
In Vitro Model Squamous cell carcinoma UM-SCC-6 cells CVCL_7773
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 6.25 ug/mL - 12.5 ug/mL Positive EGFR expression (EGFR +++/++)
Method Description
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model Squamous cell carcinoma UM-SCC-6 cells CVCL_7773
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 12.50 ug/mL Positive EGFR expression (EGFR +++/++)
Method Description
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 12.50 ug/mL Positive EGFR expression (EGFR +++/++)
Method Description
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model Lung large cell carcinoma NCI-H1299 cells CVCL_0060
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100.00 ug/mL Negative EGFR expression (EGFR -)
Method Description
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model Lung squamous cell carcinoma NCI-H520 cells CVCL_1566
References
Ref 1 Cetuximab-Triptolide Conjugate Suppresses the Growth of EGFR-Overexpressing Lung Cancers through Targeting RNA Polymerase II. Mol Ther Oncolytics. 2020 Jul 6;18:304-316. doi: 10.1016/j.omto.2020.07.001. eCollection 2020 Sep 25.

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