General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0KLOAQ
ADC Name
scFv(trastuzumab)-PE38KDEL
Synonyms
scFv(trastuzumab) PE38KDEL
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Gastric cancer [ICD11:2B72]
Investigative
Antibody Name
Trastuzumab scFv
 Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
 Antigen Info 
Payload Name
Pseudomonas exotoxin PE38
 Payload Info 
Therapeutic Target
Eukaryotic elongation factor 2 (EEF2)
 Target Info 
Linker Name
Undisclosed
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 13
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
3
pM
NCI-N87 cells
Gastric tubular adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 13.00% (Day 3) Positive HER2 expression (HER2 +++/++)
Method Description
N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 3 and day 7 at the dosage of 0.166 mg/kg.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 3.00 pM Positive HER2 expression (HER2 +++/++)
Method Description
N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
References
Ref 1 Antibody-drug conjugates with HER2-targeting antibodies from synthetic antibody libraries are highly potent against HER2-positive human gastric tumor in xenograft models. MAbs. 2019 Jan;11(1):153-165. doi: 10.1080/19420862.2018.1541370. Epub 2018 Nov 8.

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