Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0QQDEC
ADC Name	Anti-MSLN-46 ADC
Synonyms	Anti-MSLN 46 ADC; meso-46 Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Gastric cancer [ICD11:2B72] Investigative
Drug-to-Antibody Ratio	1.9
	3D MOL	2D MOL
Antibody Name	Anti-MSLN mAb		Antibody Info
Antigen Name	Mesothelin (MSLN)		Antigen Info
Payload Name	Tetrahydroisoquinoline-based PBD dimer 17		Payload Info
Therapeutic Target	Human Deoxyribonucleic acid (hDNA)		Target Info
Linker Name	PEG2-Val-Cit-PABC		Linker Info
Conjugate Type	Bacterial transglutaminase (BTGase)-mediated site-specific conjugation (Q295).

General Information of The Activity Data Related to This ADC

Revealed Based on the Cell Line Data

Click To Hide/Show 2 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	0.02	nM	NCI-N87 cells	Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 100	nM	NCI-H187 cells	Lung small cell carcinoma

Full List of Activity Data of This Antibody-drug Conjugate

Revealed Based on the Cell Line Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MSLN expression (MSLN+++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative MSLN expression (MSLN-)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

References

Ref 1	Design, Synthesis, and Structure-Activity Relationships of Novel Tetrahydroisoquinolino Benzodiazepine Dimer Antitumor Agents and Their Application in Antibody-Drug Conjugates. J Med Chem. 2020 Nov 25;63(22):13913-13950. doi: 10.1021/acs.jmedchem.0c01385.