General Information of This Payload
Payload ID
PAY0KYHON
Name
Alpha-amanitin+Monomethyl auristatin E
Synonyms
Alpha-amanitin+Monomethyl auristatin E
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Target(s) DNA-directed RNA polymerase II subunit RPB2 (POLR2B); DNA-directed RNA polymerase III subunit RPC7 (POLR3G); Microtubule (MT)
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
WO2017089890A1 ADC78 [Investigative]
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)
0.03 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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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)
0.03 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.33 nM
High HER2 expression (HER2+++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.76 nM
High HER2 expression (HER2+++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.30 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC58 [Investigative]
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)
0.06 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   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 Inhibitory Concentration (IC50)
0.64 nM
High HER2 expression (HER2+++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.73 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.95 nM
High HER2 expression (HER2+++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.30 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Conjugates comprising self-immolative groups and methods related thereto.

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