General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0ZQLZD
ADC Name
TR1801-ADC
Synonyms
MT-8633; TR 1801 ADC; TR1801-antibody drug conjugate
   Click to Show/Hide
Organization
Tanabe Research Laboratories U.S.A., Inc.
Drug Status
Phase 1
Indication
In total 3 Indication(s)
Colorectal cancer [ICD11:2B91]
Phase 1
Gastric cancer [ICD11:2B72]
Phase 1
Head and neck cancer [ICD11:2B60-2B6E]
Phase 1
Drug-to-Antibody Ratio
1.96
Structure
Antibody Name
TR1801Ab
 Antibody Info 
Antigen Name
Hepatocyte growth factor receptor (MET)
 Antigen Info 
Payload Name
SG3199
 Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
 Target Info 
Linker Name
Mal-PEG8-Val-Ala-PABC
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
SG3249
DrugMap ID
DMGC2AT
TTD ID
DU6H8Z
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Undisclosed  NCT03859752
Phase 1
A phase 1, open label, first-in-human study of TR1801-ADC, an antibody drug conjugate (ADC), in patients with select solid tumors expressing c-met.
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 28 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 1.02
%
Colorectal cancer PDX model (PDX: CR3150)
Tumor Growth Inhibition value (TGI) 
≈ 30.2
%
Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Tumor Growth Inhibition value (TGI) 
≈ 30.4
%
Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Tumor Growth Inhibition value (TGI) 
≈ 34.8
%
Colorectal cancer PDX model (PDX: CR0126)
Tumor Growth Inhibition value (TGI) 
≈ 35.4
%
Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Tumor Growth Inhibition value (TGI) 
≈ 37.5
%
Colorectal cancer PDX model (PDX: CR3150)
Tumor Growth Inhibition value (TGI) 
≈ 44.6
%
Colorectal cancer PDX model (PDX: CR0126)
Tumor Growth Inhibition value (TGI) 
≈ 45.7
%
Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Tumor Growth Inhibition value (TGI) 
≈ 45.7
%
Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Tumor Growth Inhibition value (TGI) 
≈ 47.3
%
Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Tumor Growth Inhibition value (TGI) 
≈ 53.2
%
Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Tumor Growth Inhibition value (TGI) 
≈ 59.1
%
Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Tumor Growth Inhibition value (TGI) 
≈ 60.4
%
Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Tumor Growth Inhibition value (TGI) 
≈ 70.3
%
Colorectal cancer PDX model (PDX: CR3150)
Tumor Growth Inhibition value (TGI) 
≈ 70.8
%
Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Tumor Growth Inhibition value (TGI) 
≈ 70.9
%
Colorectal cancer PDX model (PDX: CR0126)
Tumor Growth Inhibition value (TGI) 
≈ 76.5
%
Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Tumor Growth Inhibition value (TGI) 
≈ 79.4
%
Gastric cancer PDX models (PDX: GA0152)
Tumor Growth Inhibition value (TGI) 
≈ 80.5
%
Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Tumor Growth Inhibition value (TGI) 
≈ 80.9
%
Colorectal cancer PDX model (PDX: CR0126)
Tumor Growth Inhibition value (TGI) 
≈ 81.4
%
Gastric cancer PDX models (PDX: GA3121)
Tumor Growth Inhibition value (TGI) 
≈ 89.2
%
Gastric cancer PDX models (PDX: GA0152)
Tumor Growth Inhibition value (TGI) 
≈ 95.1
%
Colorectal cancer PDX model (PDX: CR3150)
Tumor Growth Inhibition value (TGI) 
≈ 96.3
%
Gastric cancer PDX models (PDX: GA3121)
Tumor Growth Inhibition value (TGI) 
≈ 97.6
%
Gastric cancer PDX models (PDX: GA0152)
Tumor Growth Inhibition value (TGI) 
≈ 99.1
%
Gastric cancer PDX models (PDX: GA3121)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Gastric cancer PDX models (PDX: GA3121)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Gastric cancer PDX models (PDX: GA0152)
Revealed Based on the Cell Line Data
Click To Hide/Show 30 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Maximum inhibition efficiency (MIE) 
68.3
%
Detroit 562 cells
Pharyngeal squamous cell carcinoma
Maximum inhibition efficiency (MIE) 
88.8
%
NCI-H1573 cells
Lung adenocarcinoma
Maximum inhibition efficiency (MIE) 
90.5
%
SNU-16 cells
Gastric adenocarcinoma
Maximum inhibition efficiency (MIE) 
92.4
%
SW480 cells
Colon adenocarcinoma
Maximum inhibition efficiency (MIE) 
92.9
%
SW1417 cells
Colon adenocarcinoma
Maximum inhibition efficiency (MIE) 
95.2
%
NCI-H441 cells
Lung papillary adenocarcinoma
Maximum inhibition efficiency (MIE) 
95.5
%
NCI-H1373 cells
Lung adenocarcinoma
Maximum inhibition efficiency (MIE) 
97.4
%
SNU-1 cells
Gastric adenocarcinoma
Maximum inhibition efficiency (MIE) 
97.5
%
SNU-5 cells
Gastric adenocarcinoma
Maximum inhibition efficiency (MIE) 
97.6
%
NCI-H1975 cells
Lung adenocarcinoma
Maximum inhibition efficiency (MIE) 
97.8
%
MKN45 cells
Gastric adenocarcinoma
Maximum inhibition efficiency (MIE) 
98.1
%
FaDu cells
Hypopharyngeal squamous cell carcinoma
Maximum inhibition efficiency (MIE) 
98.9
%
HCT 116 cells
Colon carcinoma
Maximum inhibition efficiency (MIE) 
99.1
%
NCI-H747 cells
Cecum adenocarcinoma
Maximum inhibition efficiency (MIE) 
99.3
%
SNU-620 cells
Gastric adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
4.2
pM
NCI-H441 cells
Lung papillary adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
15.6
pM
SNU-5 cells
Gastric adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
15.8
pM
MKN45 cells
Gastric adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
190.2
pM
HCT 116 cells
Colon carcinoma
Half Maximal Inhibitory Concentration (IC50) 
197.9
pM
SNU-620 cells
Gastric adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
327.5
pM
FaDu cells
Hypopharyngeal squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
346.4
pM
NCI-H1975 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
1380
pM
SW480 cells
Colon adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
2272.7
pM
NCI-H1373 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
3230
pM
NCI-H747 cells
Cecum adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
3494
pM
SW1417 cells
Colon adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
4664
pM
SNU-16 cells
Gastric adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
11.03
nM
Detroit 562 cells
Pharyngeal squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
13.44
nM
NCI-H1573 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
24.37
nM
SNU-1 cells
Gastric adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Related Clinical Trial
NCT Number NCT03859752  Clinical Status Phase 1
Clinical Description A phase 1, open label, first-in-human study of TR1801-ADC, an antibody drug conjugate (ADC), in patients with select solid tumors expressing c-met.
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 28 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 1.02% (Day 25) High MET expression (MET+++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.

   Click to Show/Hide
In Vivo Model Colorectal cancer PDX model (PDX: CR3150)
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 30.20% (Day 28) High MET expression (MET+++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 30.40% (Day 45) Moderate MET expression (MET++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 34.80% (Day 42) Moderate MET expression (MET++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.

   Click to Show/Hide
In Vivo Model Colorectal cancer PDX model (PDX: CR0126)
Experiment 5 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 35.40% (Day 28) Moderate MET expression (MET++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Experiment 6 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 37.50% (Day 25) Moderate MET expression (MET++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.

   Click to Show/Hide
In Vivo Model Colorectal cancer PDX model (PDX: CR3150)
Experiment 7 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 44.60% (Day 42) High MET expression (MET+++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.

   Click to Show/Hide
In Vivo Model Colorectal cancer PDX model (PDX: CR0126)
Experiment 8 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 45.70% (Day 28) Moderate MET expression (MET++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Experiment 9 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 45.70% (Day 45) Negative MET expression (MET-)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Experiment 10 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 47.30% (Day 28) High MET expression (MET+++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Experiment 11 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 53.20% (Day 28) Moderate MET expression (MET++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Experiment 12 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 59.10% (Day 28) High MET expression (MET+++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Experiment 13 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 60.40% (Day 45) High MET expression (MET+++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Experiment 14 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 70.30% (Day 25) High MET expression (MET+++; IHC H-score=300)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.

   Click to Show/Hide
In Vivo Model Colorectal cancer PDX model (PDX: CR3150)
Experiment 15 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 70.80% (Day 28) High MET expression (MET+++; IHC H-score=295)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Experiment 16 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 70.90% (Day 42) Moderate MET expression (MET++; IHC H-score=173)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.

   Click to Show/Hide
In Vivo Model Colorectal cancer PDX model (PDX: CR0126)
Experiment 17 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 76.50% (Day 45) Moderate MET expression (MET++; IHC H-score=130)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Experiment 18 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 79.40% (Day 60) Moderate MET expression (MET++; IHC H-score=180)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.

   Click to Show/Hide
In Vivo Model Gastric cancer PDX models (PDX: GA0152)
Experiment 19 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.50% (Day 28) Moderate MET expression (MET++; IHC H-score=190)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.

   Click to Show/Hide
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Experiment 20 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.90% (Day 42) High MET expression (MET+++; IHC H-score=300)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.

   Click to Show/Hide
In Vivo Model Colorectal cancer PDX model (PDX: CR0126)
Experiment 21 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 81.40% (Day 60) High MET expression (MET+++; IHC H-score=300)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.

   Click to Show/Hide
In Vivo Model Gastric cancer PDX models (PDX: GA3121)
Experiment 22 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 89.20% (Day 60) Moderate MET expression (MET++; IHC H-score=190)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.

   Click to Show/Hide
In Vivo Model Gastric cancer PDX models (PDX: GA0152)
Experiment 23 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 95.10% (Day 25) High MET expression (MET+++; IHC H-score=300)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.

   Click to Show/Hide
In Vivo Model Colorectal cancer PDX model (PDX: CR3150)
Experiment 24 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.30% (Day 60) Moderate MET expression (MET++; IHC H-score=180)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.

   Click to Show/Hide
In Vivo Model Gastric cancer PDX models (PDX: GA3121)
Experiment 25 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.60% (Day 60) Moderate MET expression (MET++; IHC H-score=130)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.

   Click to Show/Hide
In Vivo Model Gastric cancer PDX models (PDX: GA0152)
Experiment 26 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.10% (Day 60) Moderate MET expression (MET++; IHC H-score=130)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.

   Click to Show/Hide
In Vivo Model Gastric cancer PDX models (PDX: GA3121)
Experiment 27 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 60) Moderate MET expression (MET++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.

   Click to Show/Hide
In Vivo Model Gastric cancer PDX models (PDX: GA3121)
Experiment 28 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 60) Moderate MET expression (MET++)
Method Description
Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.

   Click to Show/Hide
In Vivo Model Gastric cancer PDX models (PDX: GA0152)
Revealed Based on the Cell Line Data
Click To Hide/Show 30 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 68.30% High MET expression (MET+++; IHC H-score=300)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Pharyngeal squamous cell carcinoma Detroit 562 cells CVCL_1171
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 88.80% Moderate MET expression (MET++; IHC H-score=190)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung adenocarcinoma NCI-H1573 cells CVCL_1478
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 90.50% High MET expression (MET+++; IHC H-score=295)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Gastric adenocarcinoma SNU-16 cells CVCL_0076
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 92.40% Moderate MET expression (MET++; IHC H-score=190)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Colon adenocarcinoma SW480 cells CVCL_0546
Experiment 5 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 92.90% Moderate MET expression (MET++; IHC H-score=180)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Colon adenocarcinoma SW1417 cells CVCL_1717
Experiment 6 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 95.20% Moderate MET expression (MET++; IHC H-score=173)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung papillary adenocarcinoma NCI-H441 cells CVCL_1561
Experiment 7 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 95.50% Moderate MET expression (MET++; IHC H-score=180)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung adenocarcinoma NCI-H1373 cells CVCL_1465
Experiment 8 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 97.40% Moderate MET expression (MET++; IHC H-score=173)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Gastric adenocarcinoma SNU-1 cells CVCL_0099
Experiment 9 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 97.50% High MET expression (MET+++; IHC H-score=300)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Gastric adenocarcinoma SNU-5 cells CVCL_0078
Experiment 10 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 97.60% Moderate MET expression (MET++; IHC H-score=130)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 11 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 97.80% High MET expression (MET+++; IHC H-score=295)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Gastric adenocarcinoma MKN45 cells CVCL_0434
Experiment 12 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 98.10% Moderate MET expression (MET++; IHC H-score=173)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 13 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 98.90% High MET expression (MET+++; IHC H-score=295)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Colon carcinoma HCT 116 cells CVCL_0291
Experiment 14 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 99.10% High MET expression (MET+++; IHC H-score=300)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Cecum adenocarcinoma NCI-H747 cells CVCL_1587
Experiment 15 Reporting the Activity Date of This ADC [2]
Efficacy Data Maximum inhibition efficiency (MIE) 99.30% High MET expression (MET+++; IHC H-score=300)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Gastric adenocarcinoma SNU-620 cells CVCL_5079
Experiment 16 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 4.20 pM Moderate MET expression (MET++; IHC H-score=173)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung papillary adenocarcinoma NCI-H441 cells CVCL_1561
Experiment 17 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 15.60 pM High MET expression (MET+++; IHC H-score=300)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Gastric adenocarcinoma SNU-5 cells CVCL_0078
Experiment 18 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 15.80 pM High MET expression (MET+++; IHC H-score=295)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Gastric adenocarcinoma MKN45 cells CVCL_0434
Experiment 19 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 190.20 pM High MET expression (MET+++; IHC H-score=295)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Colon carcinoma HCT 116 cells CVCL_0291
Experiment 20 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 197.90 pM High MET expression (MET+++; IHC H-score=300)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Gastric adenocarcinoma SNU-620 cells CVCL_5079
Experiment 21 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 327.50 pM Moderate MET expression (MET++; IHC H-score=173)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Hypopharyngeal squamous cell carcinoma FaDu cells CVCL_1218
Experiment 22 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 346.40 pM Moderate MET expression (MET++; IHC H-score=130)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 23 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1380.00 pM Moderate MET expression (MET++; IHC H-score=190)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Colon adenocarcinoma SW480 cells CVCL_0546
Experiment 24 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 2272.70 pM Moderate MET expression (MET++; IHC H-score=180)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung adenocarcinoma NCI-H1373 cells CVCL_1465
Experiment 25 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 3230.00 pM High MET expression (MET+++; IHC H-score=300)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Cecum adenocarcinoma NCI-H747 cells CVCL_1587
Experiment 26 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 3494.00 pM Moderate MET expression (MET++; IHC H-score=180)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Colon adenocarcinoma SW1417 cells CVCL_1717
Experiment 27 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 4664.00 pM High MET expression (MET+++; IHC H-score=295)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Gastric adenocarcinoma SNU-16 cells CVCL_0076
Experiment 28 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 11.03 nM High MET expression (MET+++; IHC H-score=300)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Pharyngeal squamous cell carcinoma Detroit 562 cells CVCL_1171
Experiment 29 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 13.44 nM Moderate MET expression (MET++; IHC H-score=190)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Lung adenocarcinoma NCI-H1573 cells CVCL_1478
Experiment 30 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 24.37 nM Moderate MET expression (MET++; IHC H-score=173)
Method Description
Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model Gastric adenocarcinoma SNU-1 cells CVCL_0099
References
Ref 1 A Phase 1, Open Label, First-in-human Study of TR1801-ADC, an Antibody Drug Conjugate (ADC), in Patients With Select Solid Tumors Expressing c-Met
Ref 2 TR1801-ADC: a highly potent cMet antibody-drug conjugate with high activity in patient-derived xenograft models of solid tumors. Mol Oncol. 2020 Jan;14(1):54-68.

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