Linker Information

General Information of This Linker
Linker ID
LIN0XVNNP
Linker Name
Vinylsulfonamide based linker 16
Linker Type
Flexible dual-reactive (thiol) linker
Antibody-Linker Relation
Cleavable
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
EGFR ADC-22 [Investigative]
 ADC Info 
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) ≈ 0.00% (Day 40) Negative EGFR expression (EGFR -)
Method Description
After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 NCI-H2228 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model NCI-H2228 CDX model
In Vitro Model Lung adenocarcinoma NCI-H2228 cells CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.65% (Day 40) Positive EGFR expression (EGFR +++/++)
Method Description
After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 HCC827 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model HCC827 CDX model
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
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)
0.50 nM±0.10 nM
Positive EGFR expression (EGFR +++/++)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500 nM Negative EGFR expression (EGFR -)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model Lung adenocarcinoma NCI-H2228 cells CVCL_1543
HER2 ADC-19 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.80 nM±1.40 nM
Positive HER2 expression (HER2 +++/++)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
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 Inhibitory Concentration (IC50) > 500 nM Negative HER2 expression (HER2 -)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500 nM Negative HER2 expression (HER2 -)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500 nM Negative HER2 expression (HER2 -)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Divinylsulfonamides enable the construction of homogeneous antibody-drug conjugates. Bioorg Med Chem. 2020 Dec 1;28(23):115793. doi: 10.1016/j.bmc.2020.115793. Epub 2020 Oct 6.

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