General Information of This Payload
Payload ID
PAY0ZVLSS
Name
Pseudomonas exotoxin PE24
Synonyms
Pseudomonas exotoxin PE24
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Target(s) Eukaryotic elongation factor 2 (EEF2)
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half-maximal effective concentration (EC50) 944500 nM
A431 cells
Skin squamous cell carcinoma
CVCL_0037 
[1]
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
A43-PE24 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 50.00% (Day 48) Positive GPC3 expression (GPC3+++/++)
Method Description
A43-PE24 induces efficient tumor cell killing in cell line-derived models of immunotherapy of hepatocellular carcinoma cells.
In Vivo Model Hepatocellular carcinoma CDX model
In Vitro Model Hepatocellular carcinoma Hepatocellular carcinoma cells Homo sapiens
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Hepatocellular carcinoma G1LG cells Homo sapiens
HN3-PE24 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 63.30% (Day 48) Positive GPC3 expression (GPC3+++/++)
Method Description
HN3-PE24 induces efficient tumor cell killing in cell line-derived models of immunotherapy of hepatocellular carcinoma cells.
In Vivo Model Hepatocellular carcinoma CDX model
In Vitro Model Hepatocellular carcinoma Hepatocellular carcinoma cells Homo sapiens
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 [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Hepatocellular carcinoma G1LG cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Pediatric hepatocellular carcinoma Hep3BLG cells Homo sapiens
C46-PE24 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 75.00% (Day 48) Positive GPC3 expression (GPC3+++/++)
Method Description
C46-PE24induces efficient tumor cell killing in cell line-derived models of immunotherapy of hepatocellular carcinoma cells.
In Vivo Model Hepatocellular carcinoma CDX model
In Vitro Model Hepatocellular carcinoma Hepatocellular carcinoma cells Homo sapiens
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Hepatocellular carcinoma G1LG cells Homo sapiens
LMB-164 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 78.15% (Day 6) Positive MSLN expression (MSLN +++/++)
Method Description
In vivo efficacy of LMB-100 and LMB-164 in an SW48 mouse xenograft model was evaluated. LMB-100 was administered i.v. at 2.5 mg/kg dose every other day for 6 days for two cycles with three days in between cycles.
In Vivo Model SW48 CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.38 ng/mL±0.08 ng/mL
Positive MSLN expression (MSLN +++/++)
Method Description
KLM-1 pancreatic adenocarcinoma cells were treated with indicated concentrations of LMB-12, LMB-100, or LMB-164 anti-MSLN targeted RITs for 72 hours before WST-8 assay of cell viability.
In Vitro Model Pancreatic ductal adenocarcinoma KLM-1 cells CVCL_5146
J80A-PE24 [Investigative]
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 [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83.30% (Day 48) Positive GPC3 expression (GPC3+++/++)
Method Description
J80A-PE24 induces efficient tumor cell killing in cell line-derived models of immunotherapy of hepatocellular carcinoma cells.
In Vivo Model Hepatocellular carcinoma
In Vitro Model Hepatocellular carcinoma Hepatocellular carcinoma cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 48) Positive GPC3 expression (GPC3+++/++)
Method Description
J80A-PE24+FGF-401 induces efficient tumor cell killing in cell line-derived models of immunotherapy of hepatocellular carcinoma cells.
In Vivo Model Hepatocellular carcinoma CDX model
In Vitro Model Hepatocellular carcinoma Hepatocellular carcinoma cells Homo sapiens
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 [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Hepatocellular carcinoma G1LG cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.90 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Pediatric hepatocellular carcinoma Hep3BLG cells Homo sapiens
I34-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Invasive breast carcinoma T-47D cells CVCL_0553
F67-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Invasive breast carcinoma T-47D cells CVCL_0553
J58-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Invasive breast carcinoma T-47D cells CVCL_0553
F5-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Invasive breast carcinoma T-47D cells CVCL_0553
G15-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Hepatocellular carcinoma G1LG cells Homo sapiens
H49-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Hepatocellular carcinoma G1LG cells Homo sapiens
A18-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Hepatocellular carcinoma G1LG cells Homo sapiens
I82-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Hepatocellular carcinoma G1LG cells Homo sapiens
J80B-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Invasive breast carcinoma T-47D cells CVCL_0553
A5-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Inhibitory Concentration 5% (IC5)
110.00 ng/mL
Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Invasive breast carcinoma T-47D cells CVCL_0553
hD7-1 (VL-VH)-PE24 [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 [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.12 nM
Positive PSMA expression (PSMA+++/++)
Method Description
The immunotoxins hD7-1 (VL-VH)-PE24 was tested for specific cytotoxic activity against PSMA-positive LNCaP and C4-2 cells.
In Vitro Model Prostate carcinoma LNCaP cells CVCL_0395
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.13 nM
Positive PSMA expression (PSMA+++/++)
Method Description
The immunotoxins hD7-1 (VL-VH)-PE24 was tested for specific cytotoxic activity against PSMA-positive LNCaP and C4-2 cells.
In Vitro Model Lymph node metastasis of prostate carcinoma LNCaP C4-2 cells CVCL_4782
RG7787 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 24 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 inhibitor 7rh in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Skin squamous cell carcinoma A-431 cells CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.40 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 inhibitor 7rh in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Breast ductal carcinoma HCC70 cells CVCL_1270
Experiment 3 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.70 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 siRNA in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Pancreatic ductal adenocarcinoma AsPC-1 cells CVCL_0152
Experiment 4 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 inhibitor 7rh in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Breast carcinoma SUM149PT cells CVCL_3422
Experiment 5 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.50 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 siRNA in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Skin squamous cell carcinoma A-431 cells CVCL_0037
Experiment 6 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.50 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 siRNA in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Peritoneal malignant mesothelioma HAY cells CVCL_N813
Experiment 7 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 inhibitor 7rh in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Pancreatic ductal adenocarcinoma KLM-1 cells CVCL_5146
Experiment 8 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 siRNA in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
Experiment 9 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Skin squamous cell carcinoma A-431 cells CVCL_0037
Experiment 10 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 inhibitor 7rh in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model . L55S cells Homo sapiens
Experiment 11 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.70 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 siRNA in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Pancreatic ductal adenocarcinoma KLM-1 cells CVCL_5146
Experiment 12 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Breast ductal carcinoma HCC70 cells CVCL_1270
Experiment 13 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 inhibitor 7rh in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Peritoneal malignant mesothelioma HAY cells CVCL_N813
Experiment 14 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with DDR1 inhibitor 7rh in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
Experiment 15 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with control si in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Pancreatic ductal adenocarcinoma KLM-1 cells CVCL_5146
Experiment 16 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model . L55S cells Homo sapiens
Experiment 17 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
11.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with control si in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Skin squamous cell carcinoma A-431 cells CVCL_0037
Experiment 18 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
11.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with control si in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Peritoneal malignant mesothelioma HAY cells CVCL_N813
Experiment 19 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
11.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Pancreatic ductal adenocarcinoma KLM-1 cells CVCL_5146
Experiment 20 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
11.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Breast carcinoma SUM149PT cells CVCL_3422
Experiment 21 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
35.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Peritoneal malignant mesothelioma HAY cells CVCL_N813
Experiment 22 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
40.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with control si in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
Experiment 23 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
40.00 ng/mL
Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity by combination with control si in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Pancreatic ductal adenocarcinoma AsPC-1 cells CVCL_0152
Experiment 24 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 ng/mL Positive MSLN expression (MSLN+++/++)
Method Description
RG7787 activity in MSLN-expressing cell lines. Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
LMB-12 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.17 ng/mL±0.08 ng/mL
Positive MSLN expression (MSLN +++/++)
Method Description
KLM-1 pancreatic adenocarcinoma cells were treated with indicated concentrations of LMB-12, LMB-100, or LMB-164 anti-MSLN targeted RITs for 72 hours before WST-8 assay of cell viability.
In Vitro Model Pancreatic ductal adenocarcinoma KLM-1 cells CVCL_5146
I88-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 ng/mL Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Hepatocellular carcinoma G1LG cells Homo sapiens
R6-PE24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 110.00 ng/mL Positive GPC3 expression (GPC3+++/++)
Method Description
Ten thousand cells were seeded in a 96-well cell culture plate (200 l per well), supplemented with purified immunotoxins at the indicated final concentrations, and incubated at 37°C for 3 days. Cell viability was determined by quantifying the enzymatic activity of the intracellular luciferase that was released by two rounds of freezing-thawing.

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In Vitro Model Hepatocellular carcinoma G1LG cells Homo sapiens
References
Ref 1 Highly Potent Immunotoxins Targeting the Membrane-distal N-lobe of GPC3 for Immunotherapy of Hepatocellular Carcinoma. J Cancer. 2022 Feb 14;13(4):1370-1384.
Ref 2 Highly Potent Immunotoxins Targeting the Membrane-distal N-lobe of GPC3 for Immunotherapy of Hepatocellular Carcinoma. J Cancer. 2022 Feb 14;13(4):1370-1384.
Ref 3 Anti-Mesothelin Recombinant Immunotoxin Therapy for Colorectal Cancer. Clin Colorectal Cancer. 2019 Sep;18(3):192-199.e1. doi: 10.1016/j.clcc.2019.06.006. Epub 2019 Jul 2.
Ref 4 In Vitro Evaluation of Humanized/De-immunized Anti-PSMA Immunotoxins for the Treatment of Prostate Cancer. Anticancer Res. 2018 Jan;38(1):61-69. doi: 10.21873/anticanres.12192.
Ref 5 Anticancer Effects of Mesothelin-Targeted Immunotoxin Therapy Are Regulated by Tyrosine Kinase DDR1. Cancer Res. 2016 Mar 15;76(6):1560-8. doi: 10.1158/0008-5472.CAN-15-2401. Epub 2015 Dec 30.

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