General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0JWSPU
ADC Name
T-PBA
Synonyms
Trastuzumab linker-payload 40
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Drug-to-Antibody Ratio
2.26
Antibody Name
Trastuzumab
 Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
 Antigen Info 
Payload Name
PBD-based payload 37b3
 Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
 Target Info 
Linker Name
Mc-Val-Ala
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
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) 
≈ 93.1
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 95.2
%
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
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) 
5.4
nM
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
56.1
nM
NCI-N87 cells
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
344.6
nM
MDA-MB-231 cells
Breast adenocarcinoma
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) ≈ 93.10% (Day 30) High HER2 expression (HER2+++)
Method Description
The efficacy of T-PBA was evaluated in two HER2-positive xenograft models at different doses and schedules. T-PBA (10 mg/kg), trastuzumab (10 mg/kg), and saline were injected by tail vein to balb/C nude mice for 0, 3, 6, and 9 days.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 95.20% (Day 30) High HER2 expression (HER2+++)
Method Description
The efficacy of T-PBA was evaluated in two HER2-positive xenograft models at different doses and schedules. T-PBA (10 mg/kg), trastuzumab (10 mg/kg), and saline were injected by tail vein to balb/C nude mice for 0, 3, 6, and 9 days.
In Vivo Model SK-OV-3 CDX model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
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) 5.40 nM High HER2 expression (HER2+++)
Method Description
Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 56.10 nM High HER2 expression (HER2+++)
Method Description
Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 344.60 nM High HER2 expression (HER2+++)
Method Description
Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
References
Ref 1 Design, Synthesis, and Bioevaluation of a Novel Hybrid Molecular Pyrrolobenzodiazepine-Anthracenecarboxyimide as a Payload for Antibody-Drug Conjugate. J Med Chem. 2022 Sep 8;65(17):11679-11702. doi: 10.1021/acs.jmedchem.2c00471. Epub 2022 Aug 18.

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