Linker Information

General Information of This Linker

Linker ID	LIN0QOUGK
Linker Name	Dibromomaleimide-PEG4
Linker Type	Flexible dual-reactive (thiol) linker
Antibody-Linker Relation	Uncleavable
Structure
Structure	3D MOL		2D MOL
Formula	C18H24Br2N4O8
Isosmiles	O=C(O)CCOCCOCCOCCOCCn1cc(CN2C(=O)C(Br)=C(Br)C2=O)nn1
InChI	InChI=1S/C18H24Br2N4O8/c19-15-16(20)18(28)24(17(15)27)12-13-11-23(22-21-13)2-4-30-6-8-32-10-9-31-7-5-29-3-1-14(25)26/h11H,1-10,12H2,(H,25,26)
InChIKey	NZKWKMBKKPXXIW-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight	584.218	Polar area	142.31
	Complexity	32	xlogp Value	0.6894
	Heavy Count	32	Rot Bonds	17
	Hbond acc	10	Hbond Donor	1

Each Antibody-drug Conjugate Related to This Linker

Full Information of The Activity Data of The ADC(s) Related to This Linker

Anti-HER2 DVD-IgG1_MMAF [Investigative]

ADC Info

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)	0.05 nM	High HER2 expression (HER2+++)
Method Description	Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO₂ for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO₂ for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Anti-HER2 DVD-IgG1-h38c2-K99C_MMAF [Investigative]

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)	0.05 nM	High HER2 expression (HER2+++)
Method Description	Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO₂ for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO₂ for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Anti-HER2 DVD-Fab_MMAF [Investigative]

ADC Info

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)	0.33 nM	High HER2 expression (HER2+++)
Method Description	Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO₂ for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO₂ for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Anti-HER2 DVD-Fab-h38c2-K99C_MMAF [Investigative]

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)	0.33 nM	High HER2 expression (HER2+++)
Method Description	Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO₂ for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO₂ for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

References

Ref 1	Sculpting a Uniquely Reactive Cysteine Residue for Site-Specific Antibody Conjugation. Bioconjug Chem. 2022 Jun 15;33(6):1192-1200.