General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0VZXAQ
ADC Name
1131-MMAE
Synonyms
1131MMAE; 1131 MMAE
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Gastric cancer [ICD11:2B72]
Investigative
Structure
Antibody Name
C-1131
 Antibody Info 
Antigen Name
Kita-kyushu lung cancer antigen 1 (CT83)
 Antigen Info 
Payload Name
Monomethyl auristatin E
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Mc-Val-Cit-PABC
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
Vedotin
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 58.8
%
MKN45 cells
Gastric adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 80.36
%
MKN45 cells
Gastric adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 83.05
%
MKN45 cells
Gastric adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 93.92
%
MKN45 cells
Gastric adenocarcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
3.87
nM
NUGC-4 cells
Gastric signet ring cell adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
5.26
nM
MKN45 cells
Gastric adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
786
nM
HGC-27 cells
Gastric carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 58.80% (Day 21) Positive KKLC1 expression (KKLC1+++/++)
Method Description
The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.3 mg/kg.
In Vivo Model Gastric cancer CDX model
In Vitro Model Gastric adenocarcinoma MKN45 cells CVCL_0434
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.36% (Day 21) Positive KKLC1 expression (KKLC1+++/++)
Method Description
The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 1 mg/kg.
In Vivo Model Gastric cancer CDX model
In Vitro Model Gastric adenocarcinoma MKN45 cells CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83.05% (Day 5) Positive KKLC1 expression (KKLC1+++/++)
Method Description
The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 3 mg/kg.
In Vivo Model Gastric cancer CDX model
In Vitro Model Gastric adenocarcinoma MKN45 cells CVCL_0434
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 93.92% (Day 21) Positive KKLC1 expression (KKLC1+++/++)
Method Description
The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2 mg/kg.
In Vivo Model Gastric cancer CDX model
In Vitro Model Gastric adenocarcinoma MKN45 cells CVCL_0434
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 3.87 nM Positive KKLC1 expression (KKLC1+++/++)
Method Description
The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Gastric signet ring cell adenocarcinoma NUGC-4 cells CVCL_3082
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 5.26 nM Positive KKLC1 expression (KKLC1+++/++)
Method Description
The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Gastric adenocarcinoma MKN45 cells CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 786.00 nM Positive KKLC1 expression (KKLC1+++/++)
Method Description
The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Gastric carcinoma HGC-27 cells CVCL_1279
References
Ref 1 An auristatin-based peptide-drug conjugate targeting Kita-Kyushu lung cancer antigen 1 for precision chemoradiotherapy in gastric cancer. Eur J Med Chem. 2022 Nov 5;241:114617.

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