Linker Information

General Information of This Linker
Linker ID
LIN0MBWZQ
Linker Name
Mc-PABC
Linker Type
Thiol-sensitive 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
Cys-linker-MMAE-based ADC 15 [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) ≈ 69.34% (Day 60) High HER2 expression (HER2 +++)
Method Description
An NCI-N87 xenograft model of HER2-positive gastric cancer cells in BALB/c nude mice was designed to assess the efficacy of ADC in vivo. The mice were given vehicle, mil40, or ADC (5 mg/kg) on days 0, 7, 14, and 21.
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) ≈ 92.21% (Day 60) High HER2 expression (HER2 +++)
Method Description
An NCI-N87 xenograft model of HER2-positive gastric cancer cells in BALB/c nude mice was designed to assess the efficacy of ADC in vivo. The mice were given vehicle, mil40, or ADC (10 mg/kg) on days 0, 7, 14, and 21.
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 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 nM
High HER2 expression (HER2 +++)
Method Description
Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.12 nM
High HER2 expression (HER2 +++)
Method Description
Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
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)
0.35 nM
High HER2 expression (HER2 +++)
Method Description
Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
97.62 nM
Negative HER2 expression (HER2-)
Method Description
Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
110.54 nM
Negative HER2 expression (HER2-)
Method Description
Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Antibody-Drug Conjugate Using Ionized Cys-Linker-MMAE as the Potent Payload Shows Optimal Therapeutic Safety. Cancers (Basel). 2020 Mar 21;12(3):744. doi: 10.3390/cancers12030744.

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